Five taccalonolides from Tacca plantaginea

The isolation of five bitter-tasting steroids as minor constituents from the Chinese medicinal plant Tacca plantaginea (Taccaceae), taccalonolides G, H, I, J, and K is described. Their structures were elucidated mainly by spectroscopic methods.     

云南红豆杉中四个新紫杉烷类二萜化合物的分离和结构鉴定

自云南红豆杉(Taxus yunnanensis ChengetL.K.Fu)树皮的二氯甲烷提取部分又分离得到7个紫杉烷类二萜和生物碱,经光谱(IR,MS,¹HNMR,¹H-¹H’COSY,¹³C-¹HCOSY)解析推定4个新的紫杉烷类二萜涨化合物的结构为5-decinnamoyl-11-acetyl-19-hydroxyl taxagifine(I),2-deacetoxy-5.decinnamoyl taxinineJ(II),1-hydroxy-2,7,9-trideacetyl baccatinI(IV)和7-xyIosyl-10-deacetyl baccatinIII(VII),3个已知的紫杉烷类二苑和生物碱是5-decinnamoyI taxinineJ(III),7-xylosyl taxol(V)和7-xylosyl cephalomannine(VI),它们是首次从该植物中得到。     

Design, synthesis and pharmacological characterization of a potent radioiodinated and photoactivatable peptidic oxytocin antagonist

Using a segment strategy, we have synthesized four iodinated photoactivatable cyclic peptidic ligands of oxytocin, bearing a beta-mercapto-betabeta-cyclopentamethylene propionic group (Pmp) on their N-terminus. All the syntheses were RP-HPLC monitored, and the compounds were HPLC purified. They were characterized by 1H NMR, MALDI-TOF, or FAB mass spectrometries. The affinities of Pmp-Tyr(Me)-Ile-Thr-Asn-Cys-Gly-Orn-Phe(3I,4N3)-NH2 (20), Pmp-Tyr-Ile-Thr-Asn-Cys-Gly-Orn-Phe(3I,4N3)-NH2 (21), Pmp-Tyr(Me)-Ile-Thr-Asn-Cys-Pro-Orn-Phe(3I,4N3)-NH2 (22), and Pmp-Tyr-Ile-Thr-Asn-Cys-Pro-Orn-Phe(3I,4N3)-NH2 (23) were evaluated as inhibition constants (K(i), in nM) for the human oxytocin receptor expressed in Chinese hamster ovary cells by displacement of a radioiodinated disulfide-cyclized antagonist (Elands et al. Eur. J. Pharmacol. 1987, 147, 197-207). The most potent of them, compound 22, was synthesized by another method in order to allow its radiolabeling by 125I. Its dissociation constant (K(d)) for the human oxytocin receptor, directly measured in saturation studies, was 0.25 +/- 0.04 nM, and its antagonist properties were determined by inactivation of phospholipase C, thus obtaining an inactivation constant (K(inact)) of 0.18 +/- 0.02 nM, evaluated by inositol phosphate accumulation. This compound is a very good tool for the mapping of peptidic antagonist binding sites in the human oxytocin receptor.     

Possible nuclear protein kinase regulation of homologous ribonucleic acid polymerases from small dense nuclei of mouse brain during morphine tolerance-dependence. Involvement of cyclic 3',5'-adenosine monophosphate

A correlation between phosphorylation and stimulation of RNA polymerases I and II by homologous nuclear protein kinase peak I from small dense nuclei of mouse brain was demonstrated. Incubation of RNA polymerase II with nuclear protein kinase peak I lowered the optimum Mg²⁺ concentration of the polymerase in the same manner as chronic morphine treatment alone did, suggesting that the change in Mg²⁺ optimum of RNA polymerase II seen during morphine tolerance-dependence may occur through changes in phosphorylation as a result of increased nuclear protein kinase activity. Experiments investigating the involvement of cyclic 3',5'-adenosine monophosphate (cAMP) in morphine tolerance-dependence demonstrated that dibutyryl-cAMP enhanced the degree of morphine tolerance developed, as reported previously [I. K. Ho, H. H. Loh and E. L. Way, J. Pharmac. exp. Ther.185, 347 (1973); I. K. Ho, H. H. Loh, H. N. Bhargava and E. L. Way, Life Sci.16, 1895 (1975)], and also enhanced the chronic morphine-induced increase in nuclear protein kinase specific activity. Alterations in the regulation of the nuclear protein kinase activity may bave subsequently affected RNA polymerase activity through phosphorylation. These results suggest that, during morphine tolerance-dependence development, cAMP may be involved in the possible nuclear protein kinase regulation of homologous RNA polymerase.     

Formation mechanism of 4,4-methylenebis(N,N-dimethylaniline) by the anodic oxidation of N,N-dimethylaniline]

Preparative constant-current electrolysis of N,N-dimethylaniline(100 mM, DMA) was carried out in dry acetonitrile containing Et4NClO4 to give N,N,N',N'-tetra-methylbenzidine(TMB) and 4,4'-methylenebis(N,N-dimethylaniline) (MDMA). In the presence of HCl, DMA was quantitatively oxidized to TMB. Formation mechanism of MDMA was discussed using the results of semi-empirical calculations that were PM3 and AM1. The proposed mechanism by Hand and coworker was ruled out and an alternative one is suggested as follows. DMA undergoes one-electron oxidation at the anode and gives the corresponding N,N-dimethylaniline cation (A). Aydroxy ion, instead of DMA, abstracts a proton from A and gives H2O and methyl(phenyl)aminomethyl radical (B). B reacts with DMA to give a 1-dimethylamino-4-(N-methyl-N-phenylamino)methyl-2,5-cyclohexadienyl radical (I). The radical I decomposes to N-methylaniline and a 1-dimethylamino-4-methylene-2,5-cyclohexadienyl radical (J). The radical J reacts with DMA to give a 1-dimethylamino-4-(4-dimethylaminobenzyl)-2,5-cyclohexadienyl radical (K), which is oxidized to MDMA by the anode.     

Development of a Testing Battery to Assess Chemical-Induced Immunotoxicity: National Toxicology Program's Guidelines for Immunotoxicity Evaluation in Mice

Development of a Testing Battery to Assess Chemical-InducedImmunotoxicity: National Toxicology Program's Guidelines forImmunotoxicity Evaluation in Mice. Luster, M. I., Munson, A.E., Thomas, P. T., Holsapple, M. P., Fenters, J. D., White,K. L., Jr., Lauer, L. D., Germolec, D. R., Rosenthal, G. J.,and Dean, J. H. (1988). Fundam. Appl. Toxicol..     

PROCEEDINGS OF THE AUSTRALASIAN SOCIETY OF CLINICAL AND EXPERIMENTAL PHARMACOLOGISTS: 9th Annual Meeting, 27–28 November 1975, Melbourne

A comparison of the effects of prostaglandins and some relaxant drugs on isolated preparations of human bronchus and guinea-pig trachea. I. S. McKnight and Diana M. Temple Effects of prostaglandins on an isolated blood vessel. J. D. Horowitz, and M. L. Mashford Prostaglandin biosynthesis in rat renal papilla: effect of catecholamines. Abraham Danon, Lucas C. T. Chang*, Alan S. Nies? and John A. Oates. Modification by capsaicin and compound 48/80 of dye leakage induced by irritants in the rat. P. T. Arvier, L. A. Chahl and R. J. Ladd The biological activity of C-terminal partial sequences of substances. P. R. W. Bury and M. L. Mashford. Purification of a vasodilator peptide in Cohn Fraction III-O of human plasma proteins. J. D. Horowitz and M. L. Mashford. The effects of clonidine on reflex sympathetic constrictor and heart rate responses evoked by a Valsalva-like manoeuvre in the unanaesthetized rabbit. P. I. Korner and P. A. Blombery The effects of acute administration of propranolol on the ‘Valsalva'-reflex sympathetic constrictor responses of the rabbit. P. A. Blombery, A. Bobik and P. I. Korner Circulatory response to haemorrhage in relation to the pattern of accompanying humoral reaction. Janina Staszewska-Barczak and G. J. Dusting Cardiovascular actions of verapamil (Isoptin) in the dog with particular reference to myo-cardial contractility. J. A. Angus*, D. R. Richmond, P. Dhumma-Upakorn, L. B. Cobbin and A. H. Goodman Effect of metoprolol on resting, post-exercise and mental stress blood pressure levels and pulse rates in hypertensive patients. Hendrika J. Waal-Manning Blind indirect measurement of blood pressure during isometric exercise and mental arithmetic. G. Nyberg The uptake and metabolism of histamine by blood vessels. A. Foldes and I. S. de la Lande Histamine H₂-receptors in human peripheral circulation. P. Chipman and W. E. Glover Histamine receptors in the coronary circulation of the dog. G. Heise, R. W. Giles and D. E. L. Wilcken Effect of phentolamine on the potentiating action of serotonin in the rabbit ear artery. P. R. Carroll, W. E. Glover and D. Morgans Effect of anaesthetics on drug responses in the cardiovascular system of greyhounds. D. L. Wilkinson and G. C. Scroop Perhexiline maleate, a new anti-anginal drug. M. L. Mashford and J. D. Horowitz Measurement of plasma nortriptyline. K. P. Maguire, B. A. Scoggins*, G. D. Burrows and B. Davies Cardiac effects of tricyclic antidepressants. P. Dumovic, G. D. Burrows, J. Vohra,* B. Davies and B. A. Scoggins? The effect of antidepressants upon cardiovascular response to noradrenaline in anaesthetized dogs. P. Dhumma-Upakorn and L. B. Cobbin Cardiovascular effects of a new antidepressant, H 102/09, in the anaesthetized dog. L. B. Cobbin and P. Dhumma-Upakorn Plasma levels of lignocaine and monoethylglycinexylidide during and after prolonged lignocaine infusions. R. L. Nation, E. U. Triggs and M. Selig Clinical pharmacology of pancuronium bromide in man. A. A. Somogyi, E. J. Triggs and C. A. Shanks Influence of temperature on the effect produced by a general anaesthetic at the postsynaptic membrane. O. P. Hamill, P. W. Gage and I. Spence Metabolism of etidocaine in man: a comparison with lignocaine. D. Morgan, J. Thomas and J. Vine Hexachlorophene absorption in premature infants and surgical patients. D. G. Ferry and M. T. S. Roberts Pharmacokinetic studies of tolmetin in man. M. L. Selley, J. Glass*, E. J. Triggs and J. Thomas The effect of non-steroidal anti-inflammatory drugs on ATP levels and histamine release from rat peritoneal cell suspension rich in mast cells. R. O. Day, J. E. Ray, G. D. Champion and D. N. Wade Single dose comparison of analgesic action of acetylsalicylate and sodium salicylate in rheumatoid arthritis. G. D. Champion, R. O. Day, N. Fagan, G. G. Graham, A. L. Haski, L. J. Hills, B. McManus and P. D. Paull The pharmacokinetics of salicylate in patients with rheumatoid arthritis. G. Graham, G. D. Champion, R. O. Day and P. D. Paull The effect of enteric coating of aspirin tablets on occult gastrointestinal blood loss. G. D. Champion, A. B. Corrigan, R. O. Day, G. C. Graham, A. Haski, J. Hewson, G. Howe* and P. D. Paull Serum salicylate levels in patients receiving a continuous dosage regime of different acetylsalicylate preparations. P. J. Keary, M. R. Laurent and D. G. Ferry Naproxen-aspirin drug interactions studied with response surface analysis. F. W. Stitt* and J. H. Vaughan? α-Methyldopamine as a false transmitter in the corpus striatum. E. L. Conway, B. Jarrott and W. J. Louis Pharmacokinetics of clonazepam in man. J. M. Bradfield, G. A. Smith, J. H. Tyrer and M. J. Eadie The elimination kinetics of diphenylhydantoin. W. D. Hooper, F. Bochner, J. H. Tyrer and M. J. Eadie Bioavailability of carbamazepine in oral dosage forms. L. M. Cotter, G. A. Smith, M. J. Eadie and J. H. Tyrer Plasma anticonvulsant concentration during pregnancy. C. M. Lander, M. J. Eadie, V. E. Edwards and J. H. Tyrer Betel nut constituents as inhibitors of GABA uptake. G. A. R. Johnston, P. KrogsgaardLarsen and A. L. Stephanson Octopamine receptors and their structural specificity. D. F. H. Dougan and D. N. Wade Distribution of haloperidol in human blood. K. F. Ilett, I. E. Hughes and L. B. Jellett Factors which influence drug metabolism in man: tolbutamide. S. M. Pond, D. J. Birkett and D. N. Wade Temperature transitions of the microsomal hydroxylation system. D. J. Birkett Receptor assays for therapeutic and side effects of spirolactones. J. W. Funder, J. Hood and J. Mercer Further characterization of two distinct drug binding sites on human serum albumin using fluorescent probes. G. Sudlow, D. N. Wade and D. J. Birkett The prevention of drug-induced blood dyscrasias. I. S. Collins Patterns of drug overdose admissions to a general hospital. K. B. McManus, S. Pond, D. N. Wade and D. J. Birkett Some β-adrenoreceptor mediated actions of NAB365 (clenbuterol) in anaesthetized guineapigs. Karin Bolimer and Stella R. O'Donnell A study of prolonged forced expiration in electroplexy. P. C. Tresise* and B. P. Murphy? Effect of oral ephedrine in asthma. J. W. Patenon*, M. E. Pickup and C. S. May Potentiation of β-receptor mediated responses to adrenaline and (-)-isoprenaline by hydrocortisone in the anaesthetized cat. E. Malta, R. G. Goldie, C. Raper and E. J. Cornish β-Adrenoceptor agonistic and antagonistic actions of compounds related to soterenol in isolated guinea-pig atrial and tracheal preparations. C. Raper and E. Malta Intravenous bolus injection of salbutamol in the management of asthma. J. W. Patenon*, S. G. Spiro, C. S. May and A. J. Johnson Effect of isoprenaline inhalation on plasma cyclic AMP levels in asthmatic subjects. P. W. Trembath, M. C. F. Pain and J. Shaw The blood-bathed everted aorta: a sensitive method for the detection of catecholamines in the circulating blood. K. K. F. Ng, S. Duffy, W. J. Louis and A. E. Doyle Extraneuronal accumulation of noradrenaline in the guinea-pig respiratory tract. Nili Saar and Stella R. O'Donnell Adrenergic innervation of the ovarian suspensory ligament in the guinea-pig. S. Mohsin, B. L. Opperman, J. N. Pennefather and D. A. Taylor The effects of angiotensin II and sar¹-ala⁸-angiotensin II (saralasin) on cyclic 3′5′-adenosine monophosphate (cAMP) content of working rat heart. G. M. Maxwell The release of purines from intrinsic neurons in the taenia coli of the guinea-pig. B. M. Paddle D. G. Satchell Increased lever pressing behaviour in adult rats after neonatal 6-hydroxydopamine treatment. D. W. Peterson and R. Laverty Effect of chronic administration of L-dopa on dopamine-β-hydroxylase in the rat. Ann J. Culvenor and B. Jarrott     

Electrophysiological properties of cardiomyocytes isolated from CYP2J2 transgenic mice

CYP2J2 is abundant in cardiac tissue and active in the biosynthesis of eicosanoids such as epoxyeicosatrienoic acids (EETs). To determine the effects of CYP2J2 and its eicosanoid products in the heart, we characterized the electrophysiology of single cardiomyocytes isolated from adult transgenic (Tr) mice with cardiac-specific overexpression of CYP2J2. CYP2J2 Tr cardiomyocytes had a shortened action potential. At 90% repolarization, the action potential duration (APD) was 30.6 +/- 3.0 ms (n = 22) in wild-type (Wt) cells and 20.2 +/- 2.3 ms (n = 19) in CYP2J2 Tr cells (p < 0.005). This shortening was probably due to enhanced maximal peak transient outward K(+) currents (I(to,peak)), which were 38.6 +/- 2.8 and 54.4 +/- 4.9 pA/pF in Wt and CYP2J2 Tr cells, respectively (p < 0.05). In contrast, the late portion of the transient outward K(+) current (I(to,280ms)), the slowly inactivating outward K(+) current (I(K,slow)), and the voltage-gated Na(+) current (I(Na)) were not significantly altered in CYP2J2 Tr cells. N-Methylsulphonyl-6-(2-proparglyloxy-phenyl)hexanamide (MS-PPOH), a specific inhibitor of EET biosynthesis, significantly reduced I(to,peak) and increased APD in CYP2J2 Tr cardiomyocytes but not in Wt cells. Intracellular dialysis with a monoclonal antibody against CYP2J2 also significantly reduced I(to,peak) and increased APD in CYP2J2 Tr cardiomyocytes. Addition of 11,12-EET or 8-bromo-cAMP significantly reversed the MS-PPOH- or monoclonal antibody-induced changes in I(to,peak) and APD in CYP2J2 Tr cells. Together, our data demonstrate that shortening of the action potential in CYP2J2 Tr cardiomyocytes is associated with enhanced I(to,peak) via an EET-dependent, cAMP-mediated mechanism.     

PROCEEDINGS OF THE AUSTRALIAN SOCIETY FOR MEDICAL RESEARCH

1. Hormones and homeostasis. J. P. Coghlan 2. Salt and water homeostasis. D. A. Denton, P. Cox, M. McKinley, J. Nelson and R. Weisinger 3. Immunoregulation. A. Basten 4. Blood volume and open-loop gain of the carotid baroreflex. J. Ludbrook, I. B. Faris and G. G. Jamieson 5. Protein synthesis in the early stages of cardiac hypertrophy. K. G. S. Clarke and L. C. Ward 6. Dexamethasone induces equivalent proteins in cystic fibrosis and normal fibroblasts. B. A. K. Khalid, G. P. Risbridger, G. L. Warne and J. W. Funder 7. Prostanoids synthesized by pericardium and epicardium. R. D. Nolan, C. J. Dusting and T. J. Martin 8. Effect of verapamil, a calcium antagonist, on collagen-induced platelet activation. P. Han, C. Boatwright and N. G. Ardlie 9. Evaluation of an Elisa technique for the measurement of anti-striational antibody. N. R. Swanson, J. Carrano and R. L. Dawkins 10. A mathematical and physical model of corneal astigmatism. Arieh Helfgott 11. Stress, glucocorticoids, dopaminergic manipulation: effects on hypothalamic, pituitary and plasma immunoreactive β-endorphin. A. T. Lim, G. C. Smith, J. A. Clements, and J. W. Funder 12. Characterization of platelet components to which antiplatelet IgG antibodies bind in idiopathic thrombocytopenic purpura. N. Kerlero de Posbo and S. L. Pfueller 13. Factor VIH-von Willebrand factor dependent platelet agglutination by ristocetin and Botrocetin: a comparative study. J. Perkin, H. H. Salem, M. A. Howard and B. G. Firkin 14. Variant von Willebrand's disease type B. M. A. Howard, H. H. Salem, K. Thomas, L. Hau, J. Perkin and B. G. Firkin 15. The measurement of thrombin by radioimmunoassay. L. Hau, H. H. Salem, I. Sloan and B. G. Firkin 16. Cryoprecipitate and factor VIII concentrate (AHF) infusion. Study of a variant von Willebrand's disease patient. K. B. Thomas, M. A. Howard and B. G. Firkin 17. Human platelet prostaglandin synthesis by immunological stimuli. B. H. Chong, H. Bull and P. A. Castaldi 18. The use of a proteolytic probe to identify the human platelet membrane receptor for factor VIH/von Willebrand factor (FVIII/vWf). M. C. Berndt, P. A. Castaldi and D. R. Phillips 19. The facilitating effects of adrenaline on platelet aggregation. H. A. Cameron and N. G. Ardlie 20. Steroid hormone receptors in the guinea-pig prostate: effect of castration. W. D. Tilley and V. R. Marshall 21. Insulin increases calcium binding to lymphocyte plasma membranes. R. White, K. Edwards, R. M. L. Murray and G. Jerums 22. Comparative survival of blastocysts transferred to syngeneic and allogeneic pseudopregnant rats. P. McCullagh 23. Insulin sensitivity alters during the menstrual cycle in normal females. D. R. Chipps, A. McElduff, D. A. Willcocks and C. J. Eastman 24. Pulsatile administration of gonadotrophin releasing hormone (GnRH). E. J. Keogh, P. F. H. Giles, J. Bertolini, S. C. McColm, S. A. Mallal, C. P. Somerville, S. A. Byrne, C. E. Martin, and A. G. Dunn, I. J. Clarke, J. Attikiouzel and T. Marshall 25. Hypothalamic control of prolactin release in patients with pathological hyperprolactinaemia. K. Ho, G. A. Smythe and L. Lazarus 26. Effect of exercise on blood glucose and glucose flux in diabetics during insulin infusion. D. J. Chisholm, D. E. James, E. W. Kraegen, A. B. Jenkins and M. Hewitt 27. Effect of hyperinsulinaemia and glucose administration on glucose flux during exercise in man. A. B. Jenkins, D. J. Chisholm, D. E. James and E. W. Kraegen 28. Monoclonal antibodies against components of the platelet surface membrane. H. Zola, P. J. McNamara, I. G. R. Beckman, D. A. Brooks, P. J. Macardle, J. Bradley, K. Goodall and A. S. Gallus 29. Purine synthesis in human peripheral lymphocytes and in B and T lymphocytes. R. Gordon, C. Counsilman, S. Ross, D. Scott, and B. Emmerson 30. Recovery of prostaglandin synthetic activity in rat platelets and aortic rings after aspirin. Helen Bull, M. Greaves and P. A. Castaldi 31. A receptor for ferritin on hepatocytes. U. Mack, L. W. Powell and J. W. Halliday 32. Ferritin synthesis in peripheral blood monocytes in iron overload. M. L. Bassett, J. W. Halliday and L. W. Powell 33. Biochemical characterization of platelet transglutaminase. G. W. Lynch and S. L. Pfueller 34. Platelet release products and activation of phagocytosis by human monocytes and polymorphs. H. Sakamoto, F. Firkin and C. Chesterman 35. Tissue tonometry: a non-invasive means of quantifying tissue changes in lymphoedematous extremities. N. B. Piller and L. Clodius 36. Changes in cell cycle kinetic parameters and cloning efficiency during growth of MCF 7 cells. R. E. Hall, C. A. Rugg, I. W. Taylor and R. L. Sutherland 37 . Purification of fetal thymidine kinase and some physical properties. L. Cosgrove, T. E. Gan and M. B. Van Der Weyden 38. Impaired stimulation of fibroblast growth by diabetic rat serum. L. J. Murphy and L. Lazarus 39. Labile proteins regulate entry into and exit from S phase in normal cells but not in adenovirus infected cells. A. W. Braithwaite 40. Epidermal growth factor stimulates mitogenesis in normal and malignant osteoblast-like cells. K. W. Ng, M. Niall, N. C. Partridge and T. J. Martin 41. Selective activation of cyclic AMP-dependent protein kinase by hormones in normal and malignant cells. S. A. Livesey, B. E. Kemp, N. C. Partridge and T. J. Martin 42. Processing of epidermal growth factor and calcitonin by T47D breast cancer cells. D. M. Findlay, K. W. Ng and M. Niall 43. Changes in prostacyclin production in the pulmonary circulation of adult mice in response to epidermal growth factor (EGF). H. M. Godfrey, M. Niall and T. J. Martin 44. Development of a fluorescent assay for histamine receptors type 1 and 2 on mouse spleen and human blood leucocytes: relation to T suppressor cells. Tein Bao Wang, S. Hunter and D. G. Jose 45. The use of cyclosporin-A as prophylaxis for graft versus host disease after allogeneic bone marrow transplantation in man. Kerry Atkinson, Robert Short, J. C. Biggs and Bone Marrow 46. Allotransplantation of fetal mouse pancreas. C. J. Simeonovic and K. J. Lafferty 47. Cellular immune function in patients treated with cyclosporin-A. G. Haran, B. Hall, G. G. Duggin, D. J. Tiller, A. G. R. Sheil and J. S. Horvath 48. Tolerance in non-immunosuppressed mice carrying long term allografts. S. J. Prowse and K. J. Lafferty 49. Studies of alloimmune responsiveness in rats treated with cyclosporin-A to prolong cardiac allograft survival. M. Jelbart, B. M. Hall, and S. Dorsch 50. Collection of stem cells from peripheral blood in early remission in acute non-lymphoblastic leukaemia (ANLL). D. N. Haylock, J. K. Jedani and C. A. Juttner 51. B-Cell monoclonality. A useful immunofluorescent parameter in the diagnosis of non-Hodgkin's Lymphoma. J. Hendrie, P. J. Zilko, G. Sterrett, R. Warren, R. Dawkins and S. Gerovich 52. Increased calcium permeability of cold-stored erythrocytes. J. S. Wiley, K. E. McCulloch and D. S. Bowden 53. High level of circulating progenitor cells in early remission from acute leukaemia. D. N. Haylock, M. A. Kirkland, J. K. Jedani and C. A. Juttner 54. Hexadimethrine bromide (polybrene) markedly enhances the adsorption of primate retroviruses onto a canine thymus cell line (Cf2Th). R. J. Coelen and D. G. Jose 55. Studies of structure and function in acquired platelet disorders. P. A. Castaldi, W. Booth, M. C. Berndt, H. Bull, M. Greaves and C. Gregory 56. Differences in the discrete bands of isoelectric focusing patterns in a comparison of four commercially available ampholytes. R. W. Blunden and R. J. Kimber 57. Detection of cystic fibrosis protein by isoelectric focusing. M. L. Bassett, S. A. Mack, B. E. Cham and R. W. Shepherd 58. Inhibition of pyruvate carboxylase by the antibacterial protein, avidin. R. G. Duggleby, P. V. Attwood, J. C. Wallace and D. B. Keech 59. The isolation and some properties of a plasma cholesteryl ester exchange protein. M. Abbey, G. D. Calvert and G. H. White 60. Variants of human transketolase. M. J. Kaczmarek and P. F. Nixon 61. The production of mononuclear cell factors (MCF) depressing collagen synthesis by human dermal fibroblasts. Prue Hart, L. W. Powell and J. W. Halliday 62. Human deoxycytidylate deaminase: a role in (he modulation of cytosine arabinoside cytotoxicity. P. H. Ellims, A. Y. Kao and B. A. Chabner 63. N-Desmethyltamoxifen: a potent anti-cancer agent in vitro. R. R. Reddel and R. L. Sutherland 64. Effect of steroid hormones on the growth of malignant melanoma in tissue culture. P. G. Gill, N. J. De Young and A. Thompson 65. Serum β₂ microglobulin levels in acute lymphocytic leukaemia. R. J. Hogg, M. S. Rice, I. R. G. Toogood, S. J. Harris and K. F. Jureidini 66. Lack of specificity of S-adenosylhomocysteine hydrolase inactivation for toxicity in ADA deficient human lymphoblasts. G. Young, L. Hallam, I. Jack and M. B. Van Der Weyden 67 . Purine and pyrimidine enzyme markers in human lymphoid malignancies. L. Hallam, T. E. Gan and M. B. Van Der Weyden 68. The influence of diet on the metabolism of tumour bearing mice. J. A. Carman, A. M. Rofe, N. Potezny and R. A. J. Conyers 69. A new technique to study repair of DNA damage by alkylating agents. Virginia C. Griffith and D. R. Turner 70. Immunopharmacological potentiation of interleukin 2 release . P. Hersey, C. Bindon, M. Bradley and A. Edwards 71. Release of interleukin 1 (IL1) activity from cultured tumour cells. Association with la antigen expression. P. Hersey, C. Bindon and E. Murray 72. Absence of cytotoxic lymphocytes specific for autologous tumour cells in chronic lymphocytic leukaemia. A. I. Fyfe, R. W. H. Harlow and R. M. Lowenthal 73. The development and use of urease-antibody conjugates for enzyme immunoassay procedures. H. M. Chandler, J. C. Cox, K. Healey and J. G. R. Hurrell 74. Detection of immunological reactivity against soluble tumour antigen by three lymphokine-mediated techniques. W. K. Yong and W. J. Halliday 75. Enhanced release of LAF by macrophages from Babesia-infeeteA mice after stimulation by bacterial endotoxin. P. R. Wood and I. A. Clark 76. Characterization of inhibitors of the human mitogenic response found in normal serum and in sera from patients with glomerulonephritis (GN). N. Kraft, N. M. Thomson and R. C. Atkins 77. Studies of platelet membrane receptors by the use of monoclonal antibodies. B. Barlow , J. Connellan and P. Thurlow 78. Sodium transport inhibitor in proximal tubular urine during volume expansion. A. Z. Gyory and W. Willis 79. Differentiation of noradrenergic and dopaminergic systems in the kidney: evidence against significant dopaminergic innervation. B. P. McGrath, A. Lim, Karin Bode 80. Identification of renin cDNA clones by immunological techniques. D. F. Catanzaro and B. J. Morris 81. Dopamine production and excretion in the isolated perfused rat kidney. W. R. Adam and B. A. DeJong 82. Renal distribution of a monoclonal antibody to human fibronectin. W. W. Hancock, N. Kraft and R. C. Atkins 83. α-Adrenoceptors in central regions involved in blood pressure regulation in the rat . M. J. Morris, C. I. Johnston and E. A. Woodcock 84 . Release of active and inactive kallikrein from the kidney. B. H. Clappison, S. Grinblat and C. I. Johnston 85 . MK 421: a potent long acting new oral inhibitor of angiotensin converting enzyme (ACE). B. Jackson, R. Cubela and C. I. Johnston 86. Biphasic effect of paracetamol on renal prostaglandin biosynthesis and its possible role in the development of analgesic induced kidney disease. J. Mohandas, G. G. Duggan, J. S. Horvath and D. J. Tiller 87. Comparative bioavailability of two carbamazepine products. Analysis of drug and metabolite in plasma and drug in saliva. D. T. W. Hui, D. W. A. Bourne, L. McKauge and M. J. Eadie 88 . Release of lysosomal enzymes and arachidonic acid metablites from stimulated rat peritoneal macrophages. L. K. Lim, S. Alaudeen, R. L. Smith, N. H. Hunt and M. J. Weidemann 89 . Instant coffee contains potent opiate-like activity. J. H. Boublik, J. A. Clements, A. C. Her-ington, K. N. Wynne and J. W. Funder 90 . Prevention of acute paracetamol hepatotoxicity by cimetidine in the mouse in vivo. H. E. Flamer. J. Mohandas and G. G. Duggin 91 . Angiotensin II in CSF of sheep. D. T. W. Fei, S. F. Abraham, J. P. Coghlan, D. A. Denton, M. J. McKinley, B. A. Scoggins and R. S. Weisinger 92. Affinity of carbenoxolone sodium, glycyrrhetinic and glycyrrhizic acid for renal mineralocor-ticoid receptors. D. Armanini, I. Karbowiak, Z. Krozowski and J. Funder 93. Natriuresis induced by dehydration: a cerebraliy mediated homeostatic response. M. J. McKinley, D. A. Denton, J. F. Nelson, R. Park, M. H. Smith, R. S. Weisinger and R. D. Wright 94. Preparation of an enriched fraction of separated outer medullary thick ascending limbs of the loop of Henle. B. M. Rayson and S. O. Lowther 95. Specific inhibition by adrenaline of PTH stimulated adenylate cyclase in rat renal cortex. B. Murley and E. A. Woodcock 96. Ovine endometrial oestrogen receptors prior to implantation. D. Cukier, I. J. Clarke and J. K. Findlay 97. Differential effects of glucocorticoids and mineralocorticoids on the 31K precursor of ACTH and β-endorphin in the anterior and neurointermediate lobes of the rat pituitary gland. B. A. K. Khalid, A. T. Lim, D. Fraillon and J. W. Funder 98. Physiology of 4-pregnen-17α,20α-diol 3-one (17α,20αOHP) in man. J. A. Whitworth, A. Butkus, J. P. Coghlan, D. A. Denton, D. Saines and B. A. Scoggins 99. Salivary and milk glucose during the menstrual cycle and pregnancy in women. C. G. Prosser and P. E. Hartmann 100. Measurement of human chorionic gonadotrophin (hCG) in urine following in vitro fertilization and embryo transfer. M. J. Martin, K. T. Oliva, Y. P. Du Plessis and A. Lopata 101. Mode of action of tripolassium-dicitratobismuthate (‘De-Nol’): effect on glycocalyx of duodenal enterocytes. A. S. Giraud, A. S. Newton, M. G. Korman and N. D. Yeomans 102 . The effect of ethanol upon amino acid oxidation. R. Daly, J. M. Tiernan, L. E. Carrington and L. C. Ward 103. Portal vein ligation reduces cytochrome P-450 but enhances haem oxygenase activity in rat liver microsomes: a model to study regulation of hepatic P-450. G. Farrell and L. Zaluzny 104. Effect of iron stores on hepatic uptake and subcellular metabolism of transferrin-bound iron. J. W. Wilms and R. G. Batey. A. W. Morrow 105. Mercury-induced lipid peroxidation and cellular injury in isolated rat hepatocytes. N. H. Stacey and H. Kappus 106. Malnutrition and hepatic drug metabolism in cystic fibrosis: the effects of nutritional restitu tion on antipyrine half-life. R. A. Bradbear, R. W. Shepherd and W. G. E. Cooksley 107. Plasma intestinal alkaline phosphatase (IAP) is cleared rapidly by the liver. G. P. Young and D. H. Alpers 108. Inhibition of growth in a cultured human breast cancer cell (T47 D) by 1,25-dihydroxyvitamin D. R. J. Frampton, S. Omond, J. A. Eisman and T. J. Martin 109. l,25-(OH)₂Dihydroxyvitamin D₃ receptors in primary and cultured human cancer cells. L. J. Suva, R. J. Frampton, S. Omond, J. A. Eisman and T. J. Martin 110. A biologically active photoaffinity probe used in identification of the calcitonin receptor. J. M. Moseley, D. M. Findlay, T. J. Martin and J. J. Gorman 111 . Activity ratio measurements reflect intracellular activation of cyclic AMP-dependent protein kinase in osteoblasts. N. C. Partridge, B. E. Kemp, S. A. Livesey and T. J. Martin 112. Metabolism of l,25-(OH),D, by the breast cancer cell line (T47 D). E. Sher, J. A. Eisman and T. J. Martin 113. Fetal-maternal production and metabolism of gastrin in sheep. P. Chick, A. Shulkes and K. J. Hardy 114 . Preparation of a murine monoclonal antibody to human sex hormone binding globulin. I. R. Lee, L. C. Greed and J. D. Wetherall 115. The influence of HLA on serum C4 concentrations. P. Kay, C. Witt, F. T. Christiansen, R. L. Dawkins and D. Groth 116. Improvement in serum lipids on stopping smoking: a longitudinal study in normal subjects attending stop-smoking groups. I. H. Craig, P. Dwyer and L. J. Mahar 117. Analysis of C2, C4 and Bf alleles and HLA linkages and the identification of a very rare Bf allele. D. M. Groth, P. Kay, F. T. Christiansen and R. L. Dawkins 118. Chlamydial infection in HLA B27 anterior uveitis. D. Wakefield and R. Penny 119. What quantity of venom do Australian snakes inject? J. J. Morrison, J. H. Pearn and A. R. Coulter 120. High carbohydrate diets and the risk of calcium oxalate renal stone formation in the rat. H. M. James, P. L. Wigley, A. M. Rofe, R. Bais, J. B. Edwards and R. A. J. Conyers 121. Immunogenetics of rheumatoid arthritis. D. Feeney, P. J. Zilko, P. Kay and R. Dawkins 122. Government policy on medical research. M. J. R. MacKellar 123. The structure of the NH & MRC. D. de Souza 124. New developments in ultramicro-techniques for the isolation and analysis of peptides and proteins. T. W. Milton, A. J. Hearn, P. G. Paterson, S. J. Su. Stanton 125. An introduction to NMR imaging methods. J. M. Pope 126. The evolution and biosynthesis of peptide hormones. H. D. Niall 127. The role of the major histocompatibility complex (MHC) in cell-to-cell interactions. R. V. Blanden 128. Cellular and subcellular movements. I. Buckley     

Spectrum of the mu, delta- and kappa-binding sites in homogenates of rat brain

1 In homogenates of rat brain, the binding characteristics of tritiated opiates and opioid peptides were examined and the relative capacities of mu-, delta- and kappa-binding sites of the opiate receptor determined by saturation analysis.2 In competition experiments, binding of the selective mu-ligand [(3)H]-[D-Ala(2),MePhe(4),Gly-ol(5)]enkephalin at the mu-site was displaced by [D-Ala(2),D-Leu(5)]enkephalin with rather low affinity (K(I) = 12.6 nM) and more readily by the ketazocine-like compounds (-)-ethylketazocine (K(I) = 3.1 nM) and (-)-bremazocine (K(I) = 0.32 nM), which also displaced the binding of [(3)H]-[D-Ala(2),D-Leu(5)]enkephalin from the delta-site. In contrast, the binding to the kappa-site was easily displaced by ethylketazocine (1.0 nM) and bremazocine (0.37 nM) but not by the mu-ligand [D-Ala(2),MePhe(4),Gly-ol(5)]enkephalin (K(I) = 2000-3000 nM) or the delta-ligand [D-Ala(2),D-Leu(5)]enkephalin (K(I) > 20,000 nM).3 The dissociation equilibrium constant (K(D)) and the binding capacity (pmol/g) of the mu-binding site were determined with the selective mu-ligand [(3)H]-[D-Ala(2),MePhe(4),Gly-ol(5)]enkephalin. For the delta-site, [(3)H]-[D-Ala(2),D-Leu(5)]enkephalin was used in the presence of unlabelled [D-Ala(2),MePhe(4),Gly-ol(5)]enkephalin in order to suppress cross-reactivity to the mu-binding site. For the estimation of kappa-binding, [(3)H]-(+/-)-ethylketazocine or [(3)H]-(-)-bremazocine were used in the presence of unlabelled mu- and delta-ligands for the suppression of cross-reactivities to the mu- and delta-binding sites.4 In rat brain the capacity of the mu-binding site was 7.3 pmol/g brain, that of the delta-binding site 6.7 pmol/g brain and that of the kappa-binding site 2.0 pmol/g brain. Thus, the kappa-binding site had the lowest value whereas in the guinea-pig brain the capacity of the mu-binding site was lower than that of the delta- or kappa-binding site.     

Inhibition of gastric H+, K(+)-ATPase by chalcone derivatives, xanthoangelol and 4-hydroxyderricin, from Angelica keiskei Koidzumi

Two chalcone derivatives, xanthoangelol (1) and 4-hydroxyderricin (II) isolated from Angelica keiskei Koidzumi, inhibited pig gastric H+, K(+)-ATPase with IC50 values of 1.8 and 3.3 microM, respectively. The inhibition by I or II was competitive with respect to ATP and was non-competitive with respect to K+ I and II also inhibited K+, stimulated p-nitrophenyl phosphatase, with IC50 values of 1.3 and 3.5 microM, respectively. Proton transport in-vitro was inhibited by I or II, in a dose-dependent manner, 1 at 100 mg kg-1, i.p. significantly inhibited acid secretion and the formation of stress-induced gastric lesions. These results suggest that the antisecretory effect of 1 is due to the inhibition of gastric H+, K(+)-ATPase.     

Milbemycins, a new family of macrolide antibiotics. Structure determination of milbemycins D, E, F, G, H, J and K

The milbemycins, a group of potent, broad-spectrum antiparasitic and pesticidal agents, are architecturally novel antibiotics of 16-membered macrocyclic lactone. Seven new milbemycin analogues designed as milbemycins D, E, F, G, H, J and K were isolated from the fermentation broth of the mutant strain of Streptomyces hygroscopicus subsp. aureolacrimosus. The structural determination of these new components was made mainly by comparing with mass spectra, and 1H and 13C NMR spectra of milbemycin alpha- and beta-series previously published from our laboratory. Milbemycins D, E, F, G and H have characteristically an isopropyl side chain at C-25 which differs from the known milbemycin family bearing methyl or ethyl group at C-25. Milbemycins J and K possess a ketone group at C-5 instead of a hydroxyl or methoxy group. Apart from X-ray crystallography, the R-configuration of the hydroxyl group at C-5 could be best explained both by application of CD allylic benzoate method to the n-N, N-dimethylaminobenzoate of milbemycin D and by comparison of the specific rotation of milbemycin D itself and its acetate with the epimeric isomers at C-5.     

Differences in hydration and association of helical Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-(Val-Ala-Leu-Aib)2-OMe.xH2O in two crystalline polymorphs.

The 15-residue apolar peptide, Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-(Val-Ala-Leu-Aib)2-OMe has been crystallized from 2-propanol-water (form I). The crystal parameters for I are as follows: C74H133N15O18.2H2O, space group P2(1), a = 9.185 (6) A, b = 47.410 (3) A, c = 10.325 (9) A, beta = 91.47 (2) degrees, Z = 2, R = 6.3% for 4532 reflections observed > 3 sigma (F), resolution 0.94 A. The structure is almost completely alpha-helical with eleven 5-->1 hydrogen bonds and one 4-->1 hydrogen bond near the N-terminus. The structure has been compared with a polymorph (form II) obtained from methanol-water (Karle, I. L.; Flippen-Anderson, J. L.; Uma, K.; Sukumar, M.; Balaram, P., J. Am. Chem. Soc. 1990, 112, 9350-9356). The two forms differ in the extent of hydration; form I contains two water molecules in the head-to-tail region of helical columns, while form II is more extensively solvated, with the equivalent of 7.5 water molecules. The three-dimensional packing of helices is completely parallel in I and antiparallel in II.     

PROCEEDINGS OF THE AUSTRALIAN SOCIETY FOR MEDICAL RESEARCH

1. The pituitary-adrenal axis in the guinea-pig: studies on ACTH secretion. M.J. Martin, A.E. McClelland and J.W. Funder 2. A sensitive radioimmunoassay for human (β_hEP) and camel (β_cCEP) β-Endorphin. Judith Clements and J.W. Funder 3. Effect of leu-enkephalin on serum Cortisol levels in man. G.A. Smythe, R. McGinley, D.J. Chisholm and L. Lazarus 4. Binding of 17aOH progesterone (17aOHP) to intracellular sites within bovine liver. J.W. Barlow and J. Funder 5. Studies on the modes of action of tamoxifen, a potent oestrogen antagonist. M.S. Foo and R.L. Sutherland 6. Angiotensinogen in liver cells: localization by immunocytochemistry. Brian J. Morris, Harriet S. Iwamoto and Ian A. Reid 7. Binding of human growth hormone (hGH) to growth hormone and prolactin receptors: effect of concanavalin A. A.C. Herington and Denise Elson 8. Parathyroid hormone and cyclic AMP metabolism in chick renal tubules. N.H. Hunt, J.K. Dawborn and T.J. Martin 9. Further studies on the factor VIII of a patient with a variant form of von Willebrand's disease. Margaret A. Howard, Lyne Hendrix and B.G. Firkin 10. Human factor VIII binding to platelets. J. Koutts and T.S. Zimmerman 11. Platelet aggregation and secretion: effects of low concentrations of heparin . N.G. Ardlie, V. Frewin, C. Boatwright and G. Schoefl 12. Basal and prostaglandin stimulated cyclic AMP levels of human platelets in normal and hypercholesterolaemic subjects. J.A. Jakubowski and N.G. Ardlie 13. Studies on the function of platelet surface antigens. J. Connellan, I. Smith, B. Barlow and P.A. Castaldi 14. Identification of platelet membrane antigens. S.L Pfueller and P. Hosseinzadeh 15. Effect of storage temperature on platelet aggregation, release and shape. S.E. Watts, J.V. Lloyd and R.J. Kimber 16. A defect in homeostasis in chronic idiopathic thrombocytopenic purpura. R.J. Trent, R.L. Clancy and V. Danis 17. Function of serum in leucocyte adherence inhibition. A.E. Maluish and W.J. Halliday 18. ¹²⁵ I labelling of macrophage plasma membrane with chloramine -T. W.A. Davies 19. Suppressor cells in chronic lymphatic leukaemia (CLL). J. Wotherspoon, P. Hodson, P. Hersey and F.W. Gunz 20. Microassay of blood histamine release in diagnosis and treatment of allergy . K.M. Taylor, S. Krilis, B.A. Baldo and A. Basten 21. Erythrocyte autoantibody production diminished by autoantibody-induced suppressor cells. N.F. Gare and K.O. Cox 22. Exacerbation of erythrocyte autoantibody production by splenectomy . K.O. Cox and J.J. Finlay-Jones 23. Prednisolone effects on monocyte chemotaxis; normal subjects and patients on long-term steroid therapy A.R. Tanner, J.W. Halliday and L.W. Powell 24. The interaction of human IgE with lymphoid cells . H. Zola 25. Stimulation of aldosterone production from zona glomerulosa cells in vitro by normal human serum . F.A.O. Mendelsohn and C. Kachel 26. Dopamine receptors in the kidney . William R. Adam and Janine Danks 27. Salt balance, haemorrhage and activation of renin in the rat kidney A. Gillies, L. Thompson and T. Morgan 28. Renal tubular magnesium handling and PTH . S. Carney, N. Wong, G. Quamme and J. Dirks 29. Studies on the mechanism of the potentiation of human vascular smooth muscle contraction by angiotensin. R.F.W. Moulds 30. Augmented circulating bradykinin following angiotensin converting enzyme (ACE) inhibition. P.G. Matthews and C.I. Johnston 31. Increased noradrenaline (NA) concentration in cerebellum and spinal cord of stroke-prone spontaneously hypertensive rats. P.R.C. Howe, J.C. Provis, M.J. West and J.P. Chalmers 32. Activation of the sympathoadrenal system during head-up tilt . M.J. Morris, B.P. McGrath, J. A. Millar and A.J. Barnett 33. Calcitonin production and action in a human cancer cell line. D.M. Findlay, M. de Luise, V.P. Michelangeli and T.J. Martin 34. Metabolic properties of osteogenic sarcoma cells . N.C. Partridge, M.J. Doyle, B.E. Kemp and V.P. Michelangeli 35. Western Australian Blood donors who lack immunoglobulin A. S. Leivers, F. Christiansen, M. French and M.G. Davey 36. Biochemistry of the cell cycle: Cell fractionation by centrifugal elutriation. A.A. Piper, C.A. McCaffery, B.K. Milthorpe, R.M. Fox and M.H.N. Tattersall 37. Proliferative defect of marrow cells in experimental aplastic anaemia (EAA) K.J. Trainor, A.A. Morley and R.S. Seshadri 38. Pyrimidine metabolism in human adenosine deaminase deficient lymphoblasts. N.F. Parker, I. Jack and M.B. van der Weyden 39. Thymidine phosphorylase deficiency in cultured human T leukaemic lymphocytes: determinant of sensitivity to pyrimidine antimetabolites. S.K. Piddington, A.A. Piper, M.H.N. Tattersall and R.M. Fox 40. ONA repair studies on human peripheral lymphocytes. D.R. Turner, A.A. Morley, J.R. Sorrell and R.S. Seshadri 41. Partial characterization of hepatitis B surface antigen subtypes with a view to development of a synthetic vaccine D.L. Peterson, I.M. Roberts and G.N. Vyas 42. Studies on HBeAg, anti-HBe and DNA polymerase in patients with and without HBs antigenemia . M.M. Newkirk, J.W. Halliday, L.W. Powell and J. Harper 43. Suppression of lymphocyte transformation by sera from patients with alcoholic liver disease. I.S. Rose, G.P. Young, F.J. Dudley and M.B. van der Weyden 44. The kinetics of hepatic antipyrine metabolism and the effect of smoking. R.A. Bradbear , W.G.E. Cooksley, L. Bass, G. Yates, E.A. McDonald and L.W. Powell 45. Metabolic activation of paracetamol. Q.J. Chensee, J. Mohandas, S. Mohammed, I. Calder, K. Healey and G.G. Duggin 46. Hepatic iron metabolism in the rat. R.G. Batey, J.P. Milsom and S. Sherlock 47. Development and application of an immunoassay for chenodeoxycholic acid by immunization with unconjugated bile acid. M. Cain, D. Souphandavong and M. Mackinnon 48. Reassessment of the cholesterol saturation of gallbladder and hepatic bile from patients with cholesterol or pigment gallstones or without gallstones. M.J. Whiting, V. Jarvinen, R.H.L. Down and J. McK. Watts 49. A switch-over in arousal during the menstrual cycle. J. Friedman and R.A. Meares 50. Handling of hypertonic sodium chloride by the ovine foetus. S. Potocnik, K.J. Hardy & E.M. Wintour 51. Immunofluorescence localization of prolactin to human foetal membranes. D.L. Healy, J. Batty, H.K. Muller and H.G. Burger 52. Steroid receptor assays in neoplastic tissues . P. Pearce, D. Allen and J.W. Funder 53. The hereditability of serum cholesterol in early childhood. T.J.C. Boulton and P. Poulis 54. Endocrine changes in transcendental meditation. A.J.W. Bevan 55. Prostaglandins, bone resorption and cancer. M. Greaves, D. Atkins, K.J. Ibbotson and T.J. Martin 56. Prostaglandins and 25-hydroxyvitamin D-la-hydroxylase. J.D. Wark, R.G. Larkins, J.A. Eisman and T.J. Martin 57. Intrarenal distribution of salicylate . R.J. Caterson and G.G. Duggin 58. The role of prostaglandins and cyclic AMP in bronchial hyperreactivity. B.R. Creese and M.A. Denborough 59. Exercise, asthma and cyclic AMP (cAMP). P.T.P. Bye, J.J. Marty, S.D. Anderson and C.P. Perry 60. Allergic reactions to aspirin in patients with chronic urticaria. S. Krilis, B.A. Baldo, R.P. Gregson and A. Basten 61. Biochemical and physical studies on muscle membranes. J.S. Sullivan, J.H. Bradbury and M.A. Denborough 62. Influence of thyroid state on metabolism in isolated myocardial cells. L.C. Read and M.N. Berry 63. Collagen and muscle protein synthesis during cardiac hypertrophy in the dog. CM. Bonnin, R.R. Taylor and M.P. Sparrow 64. The excretion of 3 methylhistidine to measure human muscle protein turnover. L.C. Ward and W.G.E. Cooksley 65. Structure, binding specificity and function of C-reactive protein (CRP). B.A. Baldo, T.C. Fletcher and A. White 66. Phytogeny of the mucous cells in vertebrate gastric mucosa. A.S. Giraud and N.D. Yeomans 67. Role of smooth muscle cells in atherogenesis. G.R. Campbell and J.H. Chamley-Campbell 68. Arterial endothelial injury and atherogenesis. G.B. Ryan 69. Platelets and atherogenesis. D.G. Penington 70. Lipoproteins-the molecular basis for epidemiological findings . P.J. Nestel 71. Glucocorticoid receptors and responses of lymphoid cells. A.W. Harris 72. The hormonal regulation of sex steroid hormone receptor levels in normal and neoplastic tissues. R.L. Sutherland 73. A review of the role of hormone receptors in clinical practice. R.L. Woods 74. Autonomic effects on cardiac electrophysiological parameters. W.F. Heddle, P. Tornos, A. Riggs, H. Rapp and A.M. Tonkin 75. Effect of blood pressure on indices of myocardial ischaemia in the dog . S.P. Lim, M.L. Wahlqvist and C.I. Johnston 76. Affect of ACTH and salt loading on blood pressure in sheep with reduced renal mass. J.A. Whitworth, J.P. Coghlan, D.A. Denton, K.J. Hardy, T.J. Humphrey and B.A. Scroggins 77. Sugar as a source of oxalate in renal stones . A.M. Rofe, R.A.J. Conyers, R. Bais and J.B. Edwards 78. Glomerular C3b receptor–a quantitative approach. L. Schrieber and R. Penny 79. The use of macroelectrodes in distal nephron transepithelial potential difference (PD) measurements. G.G. Allen and L.J. Barratt 80. Congenital dihydrofolate reductase deficiency-fact or fancy? R.J. Hayman, I. Jack, G. Tauro and M.B. Van der Weyden 81. Folate nutrition affects the distribution of liver folate conjugates. I.C. Cassady, M.J. Healy and P.F. Nixon 82. Dietary vitamin B12 deficiency–effect on hepatic metabolism of vitamin B12 and methyltetrahydrofolate. J. Owens and W.G.E. Cooksley 83. Mechanism of vitamin B12 transport in neonatal rat ileum. J. Brown, N.D. Gallagher and A.W. Morrow 84. Kinetics of serum and tissue ferritins-effect of carbohydrate content . J.W. Halliday, U. Mack and L.W. Powell 85. Intestinal immunity in bacterial gastroenteritis. J.T. La Brooy, D. Rowley and D.J.C. Shearman 86. Metabolism of low density lipoproteins in rabbits. Y.C. Ha, G.D. Calvert and P.J. Barter 87. Rabbit plasma high density lipoprotein. J.K. Savage, R.A. Yeates, A.M. Mackinnon and G.D. Calvert 88. Cholesterol transport in hyperalphalipoproteinaemia. P.J. Nestel and A. Poyser 89. A study of hypercholesterolaemia in cholestasis. D.R. Williams, A.M. Mackinnon and P.J. Barter 90. Apoprotein levels in patients with myocardial infarction. I.H. Craig, G. Bondjers, G. Fagar, S.-O. Olofsson, R. Reid, O. Wiklund, L. Wilhelmsen and C. Wilhelmnsson 91. Changes in HDL cholesterol and protein after renal transplantation. E. Savdie, J.C. Gibson, L.A. Simons and J.H. Stewart 92. Biosynthesis and chemistry of progstaglandins. J.E. Pike 93. Physiological aspects of prostaglandins. G.D. Thorburn 94. Prostacyclin: the prostaglandin of physiological importance in the cardiovascular system. G.J. Dusting 95. Prostaglandins in the pathogenesis of disease–malignant hypercalcaemia. T.J. Martin 96. The mechanism of allograft rejection. K.J. Lafferty 98. Drugs from the sea-fact not fiction. K.M. Taylor     

PROCEEDINGS OF THE AUSTRALIAN SOCIETY FOR MEDICAL RESEARCH

1. Recent advances in liver disease. L. W. Powell 2. Recent advances in viral hepatitis . I. D. Gust 3. The formation of bile . R. Smallwood 4. More specific, orally active, mineralocorticoid agonists and antagonists. W. R. Adam, J. W. Funder and S. Ulick 5. Properties of the cytoplasmic and nuclear oestrogen receptor in the guinea-pig prostate . W. D. Tilley, D. D. Keightley and V. R. Marshall 6. Interaction of the oestrogen receptor (ER) labelled with [³H]oestradiol, [³H] tamoxifen and [³H]monohydroxytamoxifen with oligo-dT-cellulose. L. C. Murphy and R. L. Sutherland 7. Uptake of ³H-1,25-dihydroxy vitamin D, by cultured breast cancer cells. E. Sher, R. J. Frampton, J. M. Moseley, and J. A. Eisman 8. Frequency of 1,25-dihydroxy vitamin D₃ receptor in human breast cancer . L. J. Suva, R. J. Frampton, J. A. Eisman and T. J. Martin 9. Ubiquity of 1,25-dihydroxy vitamin D₃ receptor in human breast cancer cells in culture. R. J. Frampton, E. Sher, J. M. Moseley, J. A. Eisman and T. J. Martin 10. Androgen receptors in the thymus gland . P. Pearce, B. A. K. Khalid, and J. W. Funder 11. A dual action of ACTH in release of corticosterone from the rat adrenal cortex. G. R. Cam and J. R. Bassett 12. Quantitation of binding of factor VIII antigen to concanavalin A. J. Perkin, J. Koutts, B. G. Firkin, and M. A. Howard 13. Simplified immunoradiometric assay for factor VIII coagulation antigen. K. B. Thomas , M. A. Howard and J. Koutts 14. Amidolytic measurement of normal prothrombin using a fraction of tiger snake venom as activator . A. Chester and G. P. M. Crawford 15. Hypercoagulation in glomerulonephritis. Evidence for in vivo activation of factor VIII . H. H. Salem, J. Koutts, J. A. Whitworth, M. A. Howard and B. G. Firkin 16. Absence of ristocetin cofactor in blood stored at 4°C without anticoagulant. J. V. Lloyd, J. A. Hondow, L. J. Tunbridge, S. E. Watts and W. J. Russell 17. Factor VIII in haemophiliacs and carriers. L. J. Tunbridge, B. M. Duncan and J. V. Lloyd 18. Antisera to human factor VIII raised in Balb/C mice. The production of monoclonal antibodies to factor VIII . D. E. Joshua, T. Exner, H. Kronenberg and K. A. Rickard 19. Immunoradiometric studies of factor VIII coagulant antigen. T. Exner, D. E. Joshua, K. A. Rickard and H. Kronenberg 20. Release of N-acetyl-β-glucosaminidase from synovial cells by PGE₂ . B. J. Clarris and J. R. E. Fraser 21. The fate of intravenously administered phosphocitrate, a potent inhibitor of calcification. G. Williams and J. D. Sallis 22. Haem enhances hexobarbital metabolism in isolated perfused liver following drug mediated destruction of cytochrome P-450. G. C. Farrell, M. A. Correia, J. L. Gollan and R. Schmid 23. The effect of cobalamin deficiency on the activities of the cobalamin dependent enzymes. T. Treston, J. S. D. Scott and W. G. E. Cooksley 24. Intracellular binding of cobalamin by liver and kidney. J. A. Owens and W. G. E. Cooksley 25. Nature of the molecular lesion in hereditary spherocytosis of man. J. S. Hill, W. H. Sawyer, G. J. Howlett and J. S. Wiley 26. Cytosine arabinoside transport in acute leukaemia. J. S. Wiley, S. P. Jones, W. H. Sawyer and A. R. P. Paterson 27. Membrane mediated control of cholesterol biosynthesis in Morris hepatoma . R. G. Gregg and P. A. Wilce 28. A seroepidemiological study of Hepatitis B carriers in Western Australia. R. G. Allen and M. G. Davey 29. The role of endogenous cholecystokinin in regulating pancreatic growth in the rat. S. J. Brand and R. G. H. Morgan 30. Effect of lymphokines on collagen synthesis by dermal fibroblasts. P. Hart, J. W. Halliday, W. G. E. Cooksley and L. W. Powell 31. Evaluation of the humoral immune response to Giardia lamblia. I. C. Roberts-Thomson, R. F. Anders and G. F. Mitchell 32. Gallstone pathogenesis - a mouse model . C. T. Kwok, W. Burnett and I. R. Hardie 33. The effect of ascorbic acid (AA) deficiency on tissue iron metabolism. D. J. Sizemore, H. P. Roeser, A. Nikles and J. W. Halliday 34. Limited response of rat small intestine to the stimuli of pregnancy. J. A. Robertson, W. A. Bye, R. M. Clarke and N. D. Gallagher 35. Nutrient availability and liver regeneration in pregnant mice. W. A. Bye and N. D. Gallagher 36. Radioimmunoassay of 6-keto-PGF_1α using an iodinated ligand. D. P. Mahoney, L. J. Beilin and A. Barden 37. Role of the capsule and intratubular pressure in measurement of single nephron glomerular filtration rate (SNGFR). A. Gillies, D. Hartupee, J. Burnett Jr and F. Knox 38. A direct radioimmunoassay for rat urinary kallikrein. B. H. Clappison and C. I. Johnston 39. ‘Pre’ forms of renin and NGF . D. F. Catanzaro and B. J. Morris 40. Inhibition of adenylate cyclase by angiotensin II in rat kidney . K. W. Molloy and E. A. Woodcock 41. Acid activation of inactive renin: plasma kallikrein is involved. J. G. McGirr and B. J. Morris 42. Urinary kallikrein excretion in experimental acute renal failure . P. G. Matthews, V. Mercuri and M. Yasujima 43. A search for ‘renopressin’ . K. J. Roper and B. J. Morris 44. Clinical evaluation of B-cell and T-regulator cell function by protein A plaque assay. B. M. Jones 45. What protects passively enhanced organ grafts from rejection? B. M. Hall 46. Influence of HLA phenotype on lymphocytotoxic autoantibody production. C. S. Witt and R. L. Dawkins 47. Structural and genetic influences on immunological responses against muscle. B. L. McDonald and R. L. Dawkins 48. Contact sensitivity to synthetic haptens: A role for in vitro analysis. T. Fetterhoff, J. Moorhead and R. L. Dawkins 49. Autoantibodies against erythrocytes also react with immunoglobulin G(Fc). K. O. Cox and D. A. Cunliffe 50. Requirement of factor VHI-Von Willebrand factor for platelet immuno injury by drug-dependent antibodies and for formation of the antigenic stimulus. P. K. Hosseinzadeh, S. L. Pfueller and B. G. Firkin 51. The relationship of platelet-associated IgG to anti-platelet antibodies. S. L. Pfueller, D. Tew, L. Cosgrove and N. Kerlero de Rosbo 52. Human progenitor cell (CFUc) kinetics following bone marrow transplantation (BMT) for acute myeloid leukaemia (AML). C. A. Juttner, D. N. Haylock and J. A. Tiddy 53. Characterization of cells producing murine leucocyte adherence inhibition factor (LAIF). T. A. Koppi and W. J. Halliday 54. Analysis of human leukaemic cell populations by flow cytometry using monoclonal antibodies. H. Zola, J. Bradley, I. G. R. Beckman, D. A. Brooks and P. J. McNamaia 55. Deoxyadenosine: Mechanism of differential toxicity to human T- and B-lymphoblasts. E. H. Tripp, I. W. Taylor and R. M. Fox 56. Mechanisms of fluorouracil cytotoxicity in cultured human T- and B-lymphocytes. A. A. Piper, B. K. Milthorpe and R. M. Fox 57. Solubilization of the ovine fetal liver receptor for multiplication-stimulating activity (MSA). P. C. Owens, M. W. Brinsmead, M. J. Waters and G. D. Thorburn 58. The inhibitory effect of ATP on blood platelet aggregation. W. J. Booth and A. J. Webber 59. Factors determining the stability of ferritin preparations. R. A. Ferris, A. M. Russo, L. W. Powell and J. W. Halliday 60. Myofibrillar protein breakdown in children with cystic fibrosis. L. C. Ward, R. Shepherd, W. G. E. Cooksley, M. Miller and B. S. Thomas 61. Recovery of a paramyxovirus-like agent from optic nerves of cats with focal demyelinat-ing lesions. R. D. Cook, G. E. Wilcox and R. L. P. Flower 62. The effect of hypoxia on the maintained firing rate of retinal ganglion cells. V. A. Alder 63. Electrophysiological estimation of nerve conduction velocity (CV) distribution. D. J. Caddy, H. Kranz and R. D. Westerman 64. The origin of fatigue during a maximal voluntary contraction (MVC). H. Kranz, A. M. Williams and D. J. Caddy 65. Measurement of the second filter delay in the guinea-pig cochlea. A. W. Gummer and B. M. Johnstone 66. Changes in flow rates in response to inhaling air conditioned to various temperatures and water vapour content at rest, during and after exercise in patients with asthma. S. D. Anderson, R. E. Schoeffel, E. Daviskas and R. Follet 67. Actin localization in human spermatozoa . F. M. Clarke and G. N. Clarke 68. Milk composition during the menstrual cycle in women . C. G. Prosser and P. E. Hartmann 69. Plasma turnover of I¹²⁵-labelled high density lipoprotein (HDL) in the rabbit . S. Day, J. Savage and M. Mackinnon 70. Secretion of high density lipoprotein (HDL) by the perfused rabbit liver. J. Savage, K. Jackson and M. Mackinnon 71. Diurnal changes in plasma lipoprotein lipids in normal and diabetic subjects. D. Calvert, L. Blight and T. Mannik 72. Preparation and characterization of lipoprotein-free plasma using a single-step adsorption method. P. Poulis and D. Calvert 73. Alpha-adrenergic receptors coupled to inhibition of adenylate cyclase in rat kidney . C. A. Olsson and E. A. Woodcock 74. Vasopressin RIA and hypercalcaemia. B. G. Robinson, P. Clifton-Bligh, S. B. Dowton, M. Wilkinson, B. J. Morris and S. Posen 75. Modulation of the renal 25 OH vitamin D 1 and 24 hydroxylase' by cyclic nucleotides. R. L. Prince, J. D. Wark and R. G. Larkins 76. Effect of calcitonin on urine concentration in the rat. S. Carney, C. Ray, L. Thomson and T. Morgan 77. Are the changes in the concentration of corticosteroid binding globulin in maternal plasma a marker of placental function? J. M. Potter and P. E. Hickman 78. Calcitonin responsive adenylate cyclase in human breast cancer cells. S. J. Lamp, D. M. Findlay, J. M. Moseley, V. P. Michelangeli and T. J. Martin 79. The plasma binding abnormality in familial euthyroid T₄ excess. J. W. Barlow, E. L. White, D. M. Hurley and J. R. Stockigt 80. Intracellular thyroid hormones in starvation. J. M. Corcoran, C. J. Eastman and V. E. Rashford 81. Characterization of arachidonic acid metabolism in several tissues in vitro. R. D. Nolan, J. Jakubowski, G. J. Dusting, M. C. Partridge and T. J. Martin 82. Cyclic nucleotide metabolism in the thymus of preleukaemic and leukaemic AKR mice. T. Evans and N. H. Hunt 83. Cyclic nucleotide metabolism and prostaglandin production in stimulated macrophages. L. K. Urn, N. H. Hunt, R. L. Smith and M. J. Weidemann 84. Deoxynucleoside triphosphate pools in megaloblastic lymphopoiesis. R. J. Hayman and M. B. Van Der Weyden 85. Thymidine kinase and thymidylate pools in folate deficient lymphoblasts. I. S. Rose, R. J. Hayman and M. B. Van Der Weyden 86. Effect of deoxyribonucleosides on deoxyribonucleoside triphosphate pools of human thymocyte subpopulations. R. F. Kefford, I. Taylor and R. M. Fox 87. Clonogenic growth of Wilms' tumour in semi-solid agar. P. J. Smith, G. A. Ablett and J. S. Sheridan 88. Tamoxifen treatment leads to an accumulation of MCF 7 cells in the Go/G1 phase of the cell cycle. R. L. Sutherland, A. M. Whybourne and I. W. Taylor 89. Experimental infection of an established human cell line (PMC9) with two primate retroviruses. R. J. Coelen, R. H. Whitehead and D.G. Jose 90. Reduced tumour growth in ketotic mice. N. Potezny, J. Carman, A. M. Rofe and R. A. J. Conyers 91. Immunofluorescent (IF) detection of hormone receptors in melanocytic tumours. A. J. Thompson, P. G. GUI, and M. G. Cook 92. Cancer cachexia: an explanation of the biochemical basis of mechanism. J. F. Williams 93. Blood pressure and metabolic effect of ACTH in patients with essential hypertension. J. A. Whitworth, D. Saines, R. Thatcher, B. A. Scoggins and J. P. Coghlan 94. Aspirin does not modify the hypotensive action of captopril in spontaneously hypertensive rats. R. Dinicolantonio, G. J. Dusting, J. S. Hutchinson and F. A. O. Mendelsohn 95. Noradrenaline release rates and neuronal uptake of noradrenaline in essential hypertension. P. W. Leonard, M. D. Esler, G. P. Jackman, H. Skews, A. Bobik, G. Jennings and P. I. Korner 96. Evidence for a non-renin pressor mechanism in 2-kidney 1-clip hypertension in the rat. P. P. B. James, K. C. Reeves, A. Tunney and R. Vandongen 97. Central 5-hydroxytryptamine and tryptophan hydroxylase in hypertensive rats. P. R. C. Howe, B. H. Stead and J. P. Chalmers 98. Effect of sex on the association between red cell ²²Na efflux and dietary sodium intake in essential hypertension. W. Fitzgibbon, J. B. Myers, T. 0. Morgan and S. Waga 99. Hybridomas - their production and applications. W. Boyle 100. Flow cytometry. I. W. Taylor 101. Computer usage - the task for medical researchers. I. Constable 102. The effect of azaserine on the pancreas of rats fed an alternating diet. R. A. Crass, R. G. H. Morgan and J. M. Papadimitriou 103. Strain differences in halothane hepatotoxicity. P. Hall, G. K. Gourlay, J. F. Adams and M. J. Cousins 104. Co-oxidation of paracetamol by prostaglandin endoperoxide synthetase in rabbit kidney . J. Mohandas, G. G. Duggin, J. S. Horvath and D. J. Tiller 105. Inhibition of theophylline metabolism by a macrolide antibiotic, erythromycin. J. T. Ahokas, C. Davies, P. J. Ravenscroft, B. T. Emmerson and J. Rydström 106. Renal functional abnormalities in experimental renal papillary necrosis (RPN) in the rat. R. A. Akelsen and G. C. Gobe 107. A histochemical study of paracetamol toxicity. M. C. Smail, K. N. Ham and I. C. Calder 108. Effect of gentamicin treatment in rats on renal brush border transport. C. Baxter, G. G. Duggin, J. S. Horvath and D. J. Tiller 109. Detection of an antigenic marker on human peripheral blood monocytes. D. A. Brooks, J. Bradley and H. Zola 110. Ecto-deoxytriphosphatase: a novel enzyme of human polymorphonuclear leukocytes and monocytes. G. H. Reid and R. M. Fox 111. Identification and characterization of bone marrow macrophages in the rat. B. G. Z. de la Hunty and J. M. P. Papadimitriou 112. An improved method for growth of human lymphocyte colonies. S. J. Alder, A. A. Morley and R. Seshadri 113. Simultaneous differential staining of permanently fixed human haemopoietic colonies. J. A. Tiddy, D. N. Haylock and C. A. Juttner 114. Tissue localization of monoclonal antimacrophage antibody by a peroxidase technique. W. W. Hancock, G. J. Becker, N. Kraft, J. Bell and R. C. Atkins 115. Monoclonal antibodies to human mononuclear phagocytes. G. J. Becker, N. Kraft, H. L. Lanyon and R. C. Atkins 116. Dynamic v. static methods for characterizing the carotid baroreflex in conscious rabbits. J. Ludbrook, I. B. Faris and G. G. Jamieson 117. New indices for electrophysiological evaluation of sinus node function in man. A. Helfgott, W. Heddle and A. M. Tonkin 118. Effect of noradrenaline uptake-blockers on noradrenaline kinetics in humans. M. Esler, G. Jackman, P. Leonard, H. Skews and A. Bobik 119. Improved diagnostic power of post-pacing sinus node sequences following atropine. W. F. Heddle, A. Helfgott and A. M. Tonkin 120. Cardiovascular reflex function in the rabbit following lesions of the ventrolateral medulla. M. J. West, W. W. Blessing and J. P. Chalmers 121. Changes in central adrenergic receptors during the development of spontaneous hypertension in the rat. M. J. Morris, E. A. Woodcock and C. I. Johnston 122. The effect of beta-adrenoceptor blockade and supplemental oxygen on endurance performance. P. T. P. Bye, S. D. Anderson, J. Alison, K. Yan and G. Johnson 123. Toxicological implications of drug biotransformation. D. J. Birkett 124. Variability in drug metabolism. F. Bochner 125. Mechanisms of drag metabolism leading to toxicity. I. C. Calder 126. New concepts on the role of GnRH in reproductive physiology. R. S. Swerdloff 127. New directions in clinical oncology. M. H. N. Tattersall 128. Muscle contraction and its relevance to medicine. M. A. Denborough 129. New concepts in haemostasis and haemostatic disorders. B. G. Firkin     

PROCEEDINGS OF THE AUSTRALASIAN SOCIETY OF CLINICAL AND EXPERIMENTAL PHARMACOLOGISTS

1. The development of the prejunctional receptor hypothesis . M.W. McCulloch, M.J. Rand and D. F. Story 2. Adrenoceptor- and cholinoceptor-mediated modulation of transmitter release at the somatic neuromuscular junction . C. Raper 3. Conditions of operation of positive and negative feedback regulation of transmitter noradrenaline release . D.F. Story and I.C. Medgett 4. Failure of a receptor blockade–a pre- and post-synaptic phenomenon . G.D.S. Hirst and T.O. Neild 5. Are radioligand assays useful for identification and characterization of prejunctional receptors? R.J. Summers and B. Jarrott 6. Prejunctional modulation of postganglionic cholinergic nerves . F. Mitchelson 7. Opiate receptor modulation of transmitter release . J.E. Olley* and A.L.A. Boura 8. Prejunctional receptors of human vascular sympathetic nerves . R.F. W. Moulds 9. Clinical implications of autonomic prejunctional receptors . J. Shaw 10. Correlations between the antihypertensive and haemodynamic effects of oxprenolol . R. Zacest, M.A. Robinson and L.L. Wilson 11. Comparison of long acting and short acting diuretics in mild essential hypertension . L.M.H. Wing, M.J. West, J.R. Graham and J.P. Chalmers 12. Effects on heart rate and blood pressure during graded exercise of beta adrenoceptor blocking drugs with and without intrinsic sympathomimetic activity (ISA) or ‘cardio-selectivity’ . G. Jennings, A. Bobik, P. Ashley, R. Newman, S. Ellet and P. Korner 13. Study of the effects of acute dosing with ac-methyl dopa on reflex autonomic tachycardia . A.J. McLean, G. Jennings and P.I. Korner 14. A study of in vitro vasoactivity of C.S.I, and the clinical state of patients who have had a subarachnoid haemorrhage . R.F.W. Moulds, C. Mylonas, R. Medcalfand D. Brownbill 15. Retrospective survey of digoxin usage . C. Corallo and K. Raymond 16. Dihydroergotamine kinetics in patients with orthostatic hypotension . A. Bobik, H. Skews, G. Jennings, M. Esler and P.I. Korner 17. Effect of probenecid on clofibrate disposition in man . J.R. Veenendaal. P.M. Brook and P.J. Meffin 18. Pharmacokinetics in human malnutrition . N. Buchanan 19. Impairment of an hepatic protective mechanism in man by food ingestion . A.J. McLean, C. Isbister, A. Bobik and F.J. Dudley 20. Carbamazepine monotherapy in epileptic patients . G.W. Mihaly and F.J.E. Vajda 21. Simultaneous determination of aspirin, salicyclic acid, salicyluric acid and gentisic acid in plasma by HPLC . R.H. Rumble and M.S. Roberts 22. Association between angiotensin conversion and prostacyclin release in isolated mesenteric vasculature of rats . G.J. Dusting and E.M. Mullins 23. Prostacyclin inhibits contractions of the rat isolated descending colon in response to field stimulation . I.R.N. Relf and A.L.A. Boura 24. Bradykinin induced spasm of the human umbilical vein is mediated via activation of phospholipase-A and potentiated by cooling . A.L.A. Boura, A.S.C. Sandford, R.J. McRae and W.A.W. Walters 25. L-Tryptophan-induced depression of α-adrenoceptor mediated vascular responses in the rat . P.L. Nolan and J.W. Caygill 26. Evidence against a physiological role of presynaptic alpha adrenoceptors in heart . J.A. Angus and P.I. Korner 27. The effect of DOCA hypertension on responses of the rat tail artery to potassium chloride and electrical stimulation . M.G. Venning and I.S. de la Lande 28. A possible histaminergic component of the clonidine withdrawal syndrome in the rat . S.J. Lewis, M.R. Fennessy and D.A. Taylor 29. Clonidine withdrawal syndrome and endogenous biogenic amines . D.A. Taylor, S.J. Lewis and M.R. Fennessy 30. The effects of sub-acute L-DOPA treatment of mice on L-DOPA-induced hyperactivity . O. Jenkins, R. Bailey, E. Crisp and D.M. Jackson 31. Chronic L-DOPA pretreatment of mice: production of dopamine receptor supersensitivity? R. Bailey, E. Crisp, D.M. Jackson and O. Jenkins 32. Accumulation of α-methylated phenolamines in rat brain after chronic administration of a-methyltyrosine . P.H. Duffield, D.F.H. Dougan, D.N. Wade and A.M. Duffield 33. Effect of unilateral lesions on octopamine and tyramine concentrations in rat striatum . D.F.H. Dougan, P.H. Duffield, D.N. Wade, A.M. Duffield and G. Paxinos 34. Effect of surgical denervation on α₁ and α₂-adrenoceptors in rat cerebral cortex . M.J. Morris, J.L. Elghozi, J.P. Dausse and P. Meyer 35. Localization of |³H|clonidine binding sites in membranes prepared from guinea pig renal cortex . G. McPherson and R.J. Summers 36. Characterization of (³H)cIonidine binding sites in membranes prepared from guinea pig spleen . R.J. Summers and G. McPherson 37. Alpha-adrenergic receptors modulate agonist affinity for beta-receptors in rat kidney membranes . E.A. Woodcock and C.A. Olsson 38. Pentobarbitone enhancement of GABA binding . M. Willow and G.A.R. Johnston 39. Stress induced changes in Leucine-enkephalin binding and plasma corticosterone in mice . M.J. Christie, P. Trisdikoon, J. Eross and G.B. Chesher 40. Duration of the analgesic effects of some opiate-like peptides following intracerebroven-tricular (i.c.v.) administration in the rat . M.J. Quinn and M.R. Fennessy 41. Relationship between δ⁹-tetrahydrocannabinol (δ⁹-THC) withdrawal behaviour and brain regional levels of histamine (HA) in the rat . A.J.M. Verberne, D.A. Taylor, S.J. Lewis and M.R. Fennessy 42. Long-term effects of a single dose of haloperidol or thioridazine on schedule induced drinking . G. Singer 44. Effect of o-methylflavinantine on contractions of the guinea-pig longitudinal muscle induced by co-axial electrical stimulation . R. Ansa-Asamoah and G.A. Starmer 45. Do endogenous purine nucleosides modulate the release of acetylcholine at the mammalian neuromuscular junction ? I. Spence 46. Effect of adrenaline on transmitter noradrenaline release . H. Majewski, M.W. McCulIoch, M.J. Rand and D.F. Story 47. Effects of tetrodotoxin on release of noradrenaline by nicotine in rabbit atria . C. Sarantos-Laska, M.W. McCulloch, D.F. Story and M.J. Rand 48. The effect of ventilatory gas composition on arachidonic acid metabolism in isolated perfused guinea-pig lungs . V. Iwanov, J. Staszewska-Barczak and G.J. Dusting 49. An isolated perfused adrenal preparation for studying adrenal catecholamine secretion . A.R. Collett and D.F. Story 50. Inhibition of nerve-mediated contractions in isolated guinea-pig ileum by 1-methyliso-guanosine, a novel purine from a sponge . D. Jamieson and P. Davis 53. β-Adrenoceptors and catecholamine-induced responses of human and porcine peripheral lung strip : Effects of uptake inhibitors. R.G. Goldie and G.M. Ellis 54. Uptake and release of N-methyl-D-aspartate by rat brain slices . J.H. Skerritt and G.A.R. Johnston 62. Receptor binding assay for detection of endogenous opioids . P.M. Lewis and J.E. Olley 63. Prospective drug utilization study of antibiotics based on blood level assays . A. Saunders and K. Raymond 57. The pharmacokinetics of chlorbutol . C. Tung, G.G. Graham, D.N. Wade and K.M. Williams 58. Effect of desmethylimipramine on the anorectic activity and tissue distribution of chlorphentermine in rats . R.F. Minchin, K.F. Ilett and B.W. Madsen 59. Effects of a new monoamine oxidase-A selective inhibitor (MD780515) on amine metabolism in the small intestine . K.F. Ilett, C.F. George and D.S. Davies 60. Hepatic elimination of sodium valproate (SV). F.J.E. Vajda, A.W. Marshall, G.W. Mihaly, R.A. Smallwood, J. Baldas and J. Phillips 61. A sensitive method for measurement of catecholamines and their metabolites in extracts of small brain areas . P.R. Rowe, R.J. Summers and P.M. Beart 62. Receptor binding assay for detection of endogenous opioids . P.M. Lewis and J.E. Olley 63. Prospective drug utilization study of antibiotics based on blood level assays . A. Saunders and K. Raymond 64. Gastric absorption of valproate in rats . N.D. Yeomans, F.J.E. Vajda and J. Baldas 65. Elimination kinetics of labetalol in severe renal failure . D.G. Ferry, A.J. Wood and R.R. Bailey 66. High pressure liquid chromatographic analysis of ranitidine. G.W. Mihaly, O.H. Drummer, A.W. Marshall, W.J. Louis and R.A. Smallwood 67. Model independent pharmacokinetics of slow intravenous infusions. K. Raymond and D.J. Morgan 68. Fate of oral hydrallazine in slow and fast acetylators. I. Cozamanis, P.A. Reece and R. Zacest 69. Pharmacokinetics of perhexiline maleate in patients with angina pectoris. J.D. Horowitz, P.M. Morris, A.J. Goble and W.J. Louis 70. The pharmacokinetics of midazolam in man. M.T. Smith, M.J. Eadie, T. O'Rourke-Brophy and T.C. Smith 71. The perinatal disposition of thiopentone. L. Wolf, D.J. Morgan, G.L. Blackman and J.D. Paull 72. Minor metabolites of 5-fluorocytosine in man. K.M. Williams, A.M. Duffield, R.K. Christopher and P.J. Finlayson 73. Steady-state bioavailability of a slow release theophylline formulation in children with acute asthma. D.J. Birkett, K. Coulthard, J.O. Miners, J.J. Grygiel, N. Grgurinovich and D. Lines 74. Protein binding of non-steroidal anti-inflammatory drugs in rheumatoid arthritis. S. Wanwimolruk, D.J. Birkett and P. Brooks 75. The measurement of mouth-caecal transit time using salicylazosulphapyridine. E.J. Begg, M. Kennedy, P.M. Chinwah and D.N. Wade 76. Mechanisms of acute hypertension and bradycardia following intracisternal 6-hydroxy-dopamine in conscious rabbits. G.A. Head and P.I. Koraer 77. Effects of dopamine on renal function and kallifrein excretion in the isolated perfused rat kidney. B.P. McGrath, P.G. Matthews, L. Leversha, P. Jablonski and B. Howden 78. A comparison of the effects of Endrallazine and Hydralazine on isolated human arteries and veins. S. Lipe, R. Medcalf, V. Iwanov and R.F.W. Moulds 79. Studies on amphetamine-induced circling in rats with substantia nigra lesions. J.S. McKenzie, S. Hannigan and A. Churchyard 80. Further studies on the peripheral antinociceptive action of morphine. G.A. Bentley, S.H. Newton and Jennifer Starr 81. Chronic haloperidol treatment of rats and a-adrenergic receptor sensitivity. A. Per ring-ton, R. Einstein and D.M. Jackson 82. Anticonvulsant activity of propranolol. Jenny Papanicolaou, F.J.E. Vajda and W.L Louis 83. Glycine and dopamine in the ventral tegmental area of the rat. A.L. Gundlach, D. McDonald and P.M. Beart 84. Effects of beta-adrenoceptor antagonists on the haemoglobin-oxygen (Hb-O) dissociation curve in vitro and in vitro. P.W. Trembath, E.A. Taylor, M. Roberts, and J. Amess 85. Clonidine analogues and hypothermia in mice. P.L. McLennar 86. Myolytic effects of Australian snake venoms in monkeys (Macaca fascicularis). S.K. Sutherland and D.G. Campbell 87. Prevention of sulphur-induced bronchoconstriction by disodium cromoglycate (DSCG) and Ketotifen. Diana M. Temple     

Cibenzoline, an ATP-sensitive K(+) channel blocker, binds to the K(+)-binding site from the cytoplasmic side of gastric H(+),K(+)-ATPase.

1. Cibenzoline, (+/-)-2-(2,2-diphenylcyclopropyl-2-imidazoline succinate, has been clinically used as one of the Class I type antiarrhythmic agents and also reported to block ATP-sensitive K(+) channels in excised membranes from heart and pancreatic beta cells. In the present study, we investigated if this drug inhibited gastric H(+),K(+)-ATPase activity in vitro. 2. Cibenzoline inhibited H(+),K(+)-ATPase activity of permeabilized leaky hog gastric vesicles in a concentration-dependent manner (IC(50): 201 microM), whereas no effect was shown on Na(+),K(+)-ATPase activity of dog kidney (IC(50): >1000 microM). Similarly, cibenzoline inhibited H(+),K(+)-ATPase activity of HEK-293 cells (human embryonic kidney cell line) co-transfected with rabbit gastric H(+),K(+)-ATPase alpha- and beta-subunit cDNAs (IC(50): 183 microM). 3. In leaky gastric vesicles, inhibition of H(+),K(+)-ATPase activity by cibenzoline was attenuated by the addition of K(+) (0.5 - 5 mM) in a concentration-dependent manner. The Lineweaver-Burk plot of the H(+),K(+)-ATPase activity shows that cibenzoline increases K(m) value for K(+) without affecting V(max), indicating that this drug inhibits H(+),K(+)-ATPase activity competitively with respect to K(+). 4. The inhibitory effect of H(+),K(+)-ATPase activity by cibenzoline with normal tight gastric vesicles did not significantly differ from that with permeabilized leaky gastric vesicles, indicating that this drug reacted to the ATPase from the cytoplasmic side of the membrane. 5. These findings suggest that cibenzoline is an inhibitor of gastric H(+),K(+)-ATPase with a novel inhibition mechanism, which inhibits gastric H(+),K(+)-ATPase by binding its K(+)-recognition site from the cytoplasmic side.     

Metabolism of kalopanaxsaponin K by human intestinal bacteria and antirheumatoid arthritis activity of their metabolites

When kalopanaxsaponin K (KPK) from Kalopanax pictus was incubated for 24 h at 37 degrees C with human intestinal microflora, KPK was mainly metabolized to kalopanaxsaponin I (KPI) via kalopanaxsaponin H (KPH) rather than via kalopanaxsaponin J (KPJ), and then transformed to kalopanaxsaponin A (KPA) and hederagenin. Bacteroides sp., and Bifidobacterium sp. and Fusobacterium sp. transformed KPK to KPI and KPA and hederagenin via KPH or KPJ. However, Lactobacillus sp. and Streptococcus sp. transformed KPK to KPI, KPA, and hederagenin only via KPJ. The metabolite KPA of KPK showed potent antirheumatoid arthritis activity.     

Decreases of voltage-dependent K^＋ currents densities in ventricular myocytes of guinea pigs by chronic oxidant stress

INTRODUCTION Intracellular K concentration plays an importantrole in the regulation of apoptosis process[1]. ExcessiveK efflux and intracellular K depletion may be respon-sible for the cell shrinkage and apoptotic death[2,3]. Cel-lular K homeostasis is maintained by K efflux and K uptake mechanism. Voltage-dependent K currents arethe major pathways for the K efflux, which indicatesthat voltage-dependent K currents are involved in theapoptosis. Several studies reported th…