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1.
Summary— KR31080 (2-butyl-5-methyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b] pyridine) is a potent inhibitor of angiotensin type 1 (AT1 ) receptors in rabbit aorta and human recombinant AT1 receptors. In the isolated rabbit thoracic aorta, KR31080 caused a nonparallel shift to the right of the concentration-response curves to angiotensin II (All) with decreased maximal response (pD'2 = 10.1 ± 0.1), but had no effect on the contractile response induced by norepinephrine. KR31080 inhibited specific [125 I]AII binding to rabbit aortic membranes (AT, receptors) and [125 I][Sar1 , Ile8 ]AII binding to human recombinant AT1 receptors in a concentration-dependent manner with IC50 values of 0.84 ± 0.08 nM and 1.92 ± 0.15 nM, respectively, but did not inhibit specific [125 I)AII binding to bovine cerebellum membranes (ÀT2 receptors). In the Scatchard analysis, KR31080 interacted with rabbit aortic AT1 receptors in a competitive manner, similar to losartan. These results demonstrate that KR31080 is a potent and AT1 selective angiotensin receptor antagonist which exerts a competitive antagonism in the [125 I]AII binding assay and insurmountable AT1 receptor antagonism in the functional study. 相似文献
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TF Leung WC Tsoi CK Li KW Chik MMK Shing PMP Yuen 《Acta paediatrica (Oslo, Norway : 1992)》1998,87(6):705-777
We describe a 15-y-old girl with Fechtner-like syndrome, who is the first Chinese reported to have this rare syndrome. She presented with left homonymous hemianopia and neuroimaging revealed haemorrhage in both parietal and occipital lobes. Peripheral blood smear showed macrothrombocytopenia and intracytoplasmic inclusion bodies inside leucocytes. Thrombocytopenia and proteinuria responded to intravenous immunoglobulin and pulsed methylprednisolone. This case illustrates that life-threatening haemorrhage can occur in patients with Fechtner syndrome. Although there was no effective treatment reported in the literature, high dose steroid and immunoglobulin seemed to be useful in our patient. Our patient also had nephritic-nephrotic syndrome with renal insufficiency, which is unusual in adolescent female patients. 相似文献
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Mamta Sharma Dorine Berriel-Cass Joseph Baran 《Infection control and hospital epidemiology》2004,25(6):468-471
OBJECTIVE: Surgical-site infection (SSI) is a serious and costly complication following coronary artery bypass graft (CABG). We analyzed surgical factors, microbiology, and complications at a 608-bed community teaching hospital to identify opportunities for prevention. METHODS: All patients undergoing CABG procedures from June 1997 through December 2000 were analyzed. Hospital records and postdischarge surveillance data were reviewed for demographics, surgical information, timing and classification of infection, microbiology, and bacteremic events. RESULTS: Of 3,443 patients undergoing CABG, sternal SSI developed in 122 (3.5%); 71 (58.2%) were classified as superficial SSI and 51 (41.8%) as deep SSI. Surgical antimicrobial prophylaxis was employed in all cases. On average, infection occurred 21.5 days (range, 4 to 315) after CABG. Most cases were diagnosed on readmission (59%); 20 cases (16%) were identified by postdischarge surveillance. Microbiological data were positive in 109 (89.3%), with a single pathogen implicated in most (86.2%). Gram-positive cocci were most frequently recovered (81%); gram-negative bacilli (17%), gram-positive bacilli (1%), and yeast (1%) were less common. Staphylococcus aureus was the most frequently isolated pathogen (49%). Bacteremia was noted in 22 instances (18%). It was significantly associated with deep SSI (P =. 002) and identified only in S. aureus cases. CONCLUSIONS: SSI complicated 3.5% of the procedures. S. aureus was implicated in most of the cases and was significantly associated with deep SSI. It was the only pathogen associated with secondary bacteremia. In addition to standard guidelines, targeted methods against S. aureus should help reduce the overall rate of SSI. 相似文献
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Five female patients and one male patient with solid and papillary epithelial neoplasms of the pancreas were examined with computed tomography (CT). The mean age of the patients was 27 years (range, 13-46 years). All cases showed well-encapsulated, round or lobulated masses consisting of both cystic and solid areas. Cystic portions showed CT numbers that suggested hemorrhagic necrosis. There were no internal septations within the masses. In three tumors located in the head of the pancreas, dilatation of the biliary tree was absent or minimal, although the masses were large. Two tumors contained calcifications. One tumor demonstrated metastatic deposits in liver and lymph nodes. Metastatic masses appeared similar to the primary pancreatic mass. Solid and papillary neoplasm of the pancreas should be the primary diagnostic consideration when characteristic CT findings are detected in a young female patient. 相似文献
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D T Baran A M Sorensen T W Honeyman R Ray M F Holick 《Journal of bone and mineral research》1990,5(5):517-524
1 alpha,25-Dihydroxyvitamin D3 rapidly increases cytosolic calcium and alters membrane phospholipid metabolism in hepatocytes. To define the causal relationship between these events, we examined the effects of 1 alpha,25-dihydroxyvitamin D3 on 32P-labeled lysophosphatidylinositol levels and cytosolic calcium as affected by pertussis toxin and 1 beta,25-dihydroxyvitamin D3, the biologically inactive analog. 32P-labeled lysophosphatidylinositol was determined by two-dimensional thin-layer chromatography. Cytosolic calcium was measured in cells loaded with quin-2AM. Within 5 min, 1 alpha,25-dihydroxyvitamin D3 increased hepatocyte cytosolic calcium by 31% (p less than 0.05) and 32P-labeled lysophosphatidylinositol by 38% (p less than 0.05). Pertussis toxin inhibited the hormone-induced rise in cytosolic calcium but not the increase in 32P-labeled lysophosphatidylinositol. Exposure to exogenous lysophosphatidylinositol for 5 min increased cytosolic calcium by 40% (p less than 0.05), an effect that was also inhibited by pertussis toxin. 1 beta,25-Dihydroxyvitamin D3 had no effect on either hepatocyte cytosolic calcium or 32P-labeled lysophosphatidylinositol but prevented the 1 alpha,25-dihydroxyvitamin D3-induced increments. The results suggest that a G protein sensitive to pertussis toxin is required for the transduction of the lysophosphatidylinositol signal but not the generation of the signal. The ability of 1 beta,25-dihydroxyvitamin D3 to inhibit the 1 alpha,25-dihydroxyvitamin D3-induced changes in phospholipids suggests that the epimer may compete with 1 alpha,25-dihydroxyvitamin D3 for an initiating receptor. 相似文献
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Vendeville B.; Baran D.; Gascon-Barre M.; Rubin E.; Luu T.; Vallieres S. 《Nephrology, dialysis, transplantation》1995,10(11):2020-2026
BACKGROUND.: Mercuric chloride (HgCl2 induces a lymphoproliferative disorderand autoimmune glomerulonephritis in Brown Norway (BN) rats.This syndrome is the consequence of T cell-dependent polyclonalB cell activation and autoantibody production. We have previouslyshown that HgCl2-induced autoimmune perturbations can be preventedin BN rats by the administration of cyclosporin A (CsA). Themost potent vitamin D3 metabolite 1,25(OH)2 D3 (Vit D3) sharescertain immunomodulatory properties with CsA. We therefore choseto compare the effects of Vit D3 to those of CsA in BN ratstreated with HgCl2 in order to establish whether Vit D3 eitheralone or in combination with CsA can attenuate an autoimmunesyndrome in vivo. METHODS.: BN rats were treated with HgCl2 according to a standard protocol.Subgroups of rats were also given CsA alone, Vit D3 or syntheticanalogues of Vit D3 alone, or combinations of both agents. Differentdoses and routes of administration were compared. The followingmarkers of disease activity were evaluated: mortality, peakproteinuria, serum IgE concentrations, and renal immunoglobulindeposition. RESULTS.: Disease activity was markedly attenuated in all rats treatedwith CsA alone. Vit D3 and certain of its synthetic analoguesadministered alone also tempered the autoimmune process, butto a lesser extent than did CsA. The effect of CsA alone wasso potent, that no additive or synergistic effects could bedemonstrated when CsA was administered in combination with VitD3. CONCLUSIONS.: Despite similar described immunomodulatory effects in vitro,CsA is clearly more effective than Vit D3 in preventing HgCl2autoimmune disease in BN rats. This suggests that there is adifference in the cellular targets of these two agents in vivo,and/or a difference in the potency with which HgCl2-triggeredimmune activation is suppressed. 相似文献
10.
Tarsometatarsal joint: anatomic details on MR images 总被引:3,自引:0,他引:3