Assay of volatile oil-cyclodextrin complexes by pyrolyzis gas-chromatography

A pyrolytic gaschromatographic process was developed for the routine assay of both cyclodextrin inclusion complexes, and for the differentiation of the mechanical mixture of the same oil with beta-cyclodextrin. The method is a direct assay of low material demand.     

The treatment of the distal epiphyseal fracture of the tibia (author's transl)

The distal epiphyseal fractures cases for 10 years period have been reported. The authors state that it is always worth-while to carry out an operation in group "B" of the Müller's scheme, while in group "A" and "C" only selected cases are worth to operate. In the 17 cases being observed till now no disturbed growth has been found.     

Experience with polychemotherapy based on cell synchronization, via intra-arterial infusions. Preoperative treatment of maxillofacial tumors]

Chemotherapy based upon cellular synchronisation via intra-arterial infusion was used in the treatment of 21 carcinomas of the maxillo-facial region. These tumours had never been treated either by surgery, nor by irradiation. This pre-operative treatment was not aimed at altering ghe indication for the type of operation decided upon at the outset. It was found that a combination of Vincristine, Bleomycine, Methotrexate and Dibromdulcide was more satisfactory than other types of chemotherapy. The most important complication of the method was a thrombosis of the common carotid.     

Naphthaquinones of Diospyros batocana

Root bark of West African tree DIOSPYROS BATOCANA H IERN, Ebenaceae, was examined. On the basis of chromatographic and spectral analysis it was shown to contain the naphtaquinones 7-methyljuglone, 2-methylnaphthazarin, biramentaceone, rotundiquinone, mamegakinone, diospyrin, diosquinone, isodiospyrin and batocanone. This last compound proved to be the (-)-enantiomer of isodiospyrin-2', 3'-epoxide. The probable existence of beta-dihydrodiospyrin, of a batocanone isomer and of an isodiospyrin diepoxide in this material is mentioned. The partial synthesis of two isomeric isodiospyrin di-epoxides is described.     

Reduced platelet MAO activity in healthy male students with blood group O

The association between the two genetic markers of affective disorders, ABO blood group system and platelet MAO (monoamine oxidase) activity was studied in 70 healthy young males. The platelet MAO activity of subjects with blood type O was significantly lower than that of subjects with blood type A and with blood types A + B AB + B together. This finding could constitute a "bridge" between the two genetic approaches to affective disorders.     

Value of angiography in hemangiopericytomas

Haemangiopericytoma is a rare type of tumour which mostly develops in the soft parts. The article reports on the manifestations of one tumour each in the thigh and pelvis. The angiogram shows displacement of the major arteries, the tumour-supplying vessels penetrate into the growth by means of one or several peduncles, and intensive coloration takes place during the parenchyma phase. However, the "typical angiographic image" was seen in one of the two cases only.     

Stimulus-evoked release of tritiated monoamines from rat periaqueductal gray slices in vitro and its receptor-mediated modulation

Summary The periaqueductal gray is a brain region of considerable interest. It is innervated by monoamine-containing neurons as well as by a variety of peptidergic fiber systems, and it participates in the regulation of various functions. Virtually nothing is known about monoamine release in the periaqueductal gray and its receptor-mediated modulation. We therefore studied the release of radioactivity from periaqueductal gray slices preloaded with tritriated monoamines, using an in vitro superfusion method.The release of radioactivity from superfused periaqueductal gray slices after preloading of the tissue with [³H]noradrenaline increased upon electrical stimulation in a frequency-dependent manner. The stimulus-evoked release of radioactivity was Ca²⁺-dependent. Clonidine reduced and yohimbine enhanced the release. The inhibition curve for the effect of clonidine was shifted to the right in the presence of 10^–6 M yohimbine. While phenylephrine, isoprenaline, SK&F 38393, quinpirole, carbachol, [Arg⁸]vasopressin, -MSH and ACTH-(1-24), at a concentration of 10^–6 M, did not influence the electrically evoked release of radioactivity, [Leu⁵]enkephalin reduced it. The selective -opioid receptor agonists [d-Ala²,NMePhe⁴,Gly-ol⁵]enkephalin and [d-Arg²,Lys⁴]-dermorphin-(1–4)-amide reduced the release of radioactivity, whereas the selective opioid receptor agonist [d-Pen²,d-Pen⁵]enkephalin and the selective K opioid receptor agonist U-69593 had no effect. In the presence of naloxone, which by itself had no effect on the release of radioactivity, the effect of [d-Arg²,Lys⁴]dermorphin-(1–4)-amide was abolished. These results show that the release of noradrenaline from periaqueductal gray slices is via a Ca²⁺-dependent. exocytotic process, and that it is modulated through ₂-adrenoceptors as well as via -opioid receptors. Though the overflow of radioactivity from slices preloaded with [3H]dopamine in the presence of desipramine was measurable, there are reasons to assume that we are dealing here with the release of tritiated catecholamines from a population of nerve endings consisting of noradrenergic and dopaminergic terminals.The release of radioactivity from periaqueductal gray slices preloaded with [³H]5-hydroxytryptamine upon elevation of the K⁺ concentration in the superfusion medium was much more pronounced than that induced by electrical stimulation. The K⁺-evoked release of radioactivity was almost completely abolished in the absence of Cat²⁺; showing that the release is via a Ca²⁺-dependent process. 5-Hydrotryptamine reduced the K⁺-evoked release of radioactivity in a concentration-dependent manner.Some of these data were presented at the XIth International Congress of Pharmacology, 1–6 July 1990, Amsterdam, The Netherlands (Eur J Pharmacol 183:408) Send offprint requests to D. H. G. Versteeg at the above address     

Sulpiride has an antiaggressive effect in mice without markedly depressing motor activity

The atypical neuroleptic, sulpiride is a selective D2 antagonist, having a preferential action on mesolimbic regions. The effects of acute and chronic treatment with sulpiride on aggressive behaviour in male mice were studied using an ethologically based analysis. It was hypothesized that sulpiride would diminish "threat" and "attack" but would not produce marked "immobility", because of the mesolimbic effect referred to above. Isolated albino male mice (experimental animals) were confronted by "standard opponents". Acutely-treated experimental animals received an intraperitoneal injection of sulpiride (20, 50 or 100 mg/kg) 30 min before testing. Chronically-treated animals received sulpiride (10, 20 or 50 mg/kg) once a day for 7 or 14 consecutive days. Acute treatment with sulpiride had an obvious antiaggressive effect, with significantly decreased time devoted to "attack" and "threat" behaviour. Although time spent in "immobility" was modestly increased, the time devoted to other motor behaviour was also increased. Chronic treatment for 1 or 2 weeks did not change any behavioural category, except "immobility". The antiaggressive action of acutely administered sulpiride is interpreted as a relatively specific dopaminergic antagonist effect and not as merely a non-specific correlate of its disruptive action on motor behaviour. The possible anxiolytic action of sulpiride is also discussed.     

Further characterization of the effects of imipramine on plateau membrane currents in guinea-pig ventricular myocytes

Summary The effects of imipramine, a tricyclic antidepressant, on action potential characteristics and plateau membrane currents were studied in isolated guineapig ventricular myocytes, using the whole cell configuration of the patch-clamp technique. Imipramine (1, 5 and 15 mol/l) decreased in a concentration-dependent manner the amplitude and shortened the duration of the action potential, but it had no effect on resting membrane potential. At all three concentrations tested, imipramine decreased the delayed outward potassium current, this effect being apparently voltage-independent since it did not modify the activation curve. Imipramine, 5 and 15 mol/l, also produced an inhibition of the peak high threshold calcium current, but did not change the shape of the current-voltage relationship or the apparent reversal potential of this current. Therefore, imipramine probably decreased the maximum available calcium conductance. However, the inward rectifying potassium current was not affected by any concentration of imipramine tested. Imipramine, 1 and 5 mol/l, shortened the duration of the action potentials elicited in the presence of the inorganic calcium channel blocker cobalt chloride, and at 5, but not at 1 mol/l, also shortened the action potentials obtained in the presence of the sodium channel blocker tetrodotoxin. Washout of imipramine completely reversed all its effects within 15 minutes. All these results suggest that imipramine at a concentration of 1 mol/l produced a shortening in action potential duration by inhibiting the late sodium current flowing during the plateau phase of the action potential. At concentrations of 5 and 15 mol/l the effect of imipramine on action potential duration can also be explained by a blocking effect on the high threshold calcium current. Send offprint requests to E. Delpón at the above address     

Effect of deltamethrin on antipyrine pharmacokinetics and metabolism in rat

The effect of deltamethrin pretreatment on the pharmacokinetics and metabolism of antipyrine was studied in male rats. The total plasma clearance of antipyrine was significantly decreased by deltamethrin pretreatment (20 mg/kg and 40 mg/kg daily for 6 days prior to antipyrine administration), while the elimination half-life at phase, the area under the concentration-time curve and the mean residence time of antipyrine were significantly increased. The magnitude of the observed changes was dose dependent. The urinary excretion of norantipyrine, 4-hydroxyantipyrine and 3-hydroxymethylantipyrine was decreased by 39%, 32% and 26%, respectively (p<0.001) in the presence of deltamethrin. In addition, the rate constants for formation of each of these metabolites were significantly decreased by an average of approximately 71%. These results suggest that deltamethrin is capable of inhibiting oxidative metabolism, a finding which could be of clinical and toxicological significance.