共查询到20条相似文献,搜索用时 0 毫秒
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H Yamamoto Y Nakamura Y Kunoh K Ichihara M Nagasaka H Asai 《Japanese journal of pharmacology》1986,41(3):283-292
Effects of (-) cis-2,3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-benz othiazepin-4-(5H ) -one hydrochloride (BTM-1086) on various experimental gastric and duodenal ulcers were studied in rats. In the pylorus-ligated ulcer, restraint and water immersion stress ulcer, and drug-induced ulcer (indomethacin, aspirin, reserpine, serotonin, cysteamine), BTM-1086 prevented the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibited the histamine-induced gastric ulcer. The inhibitory activities of BTM-1086 were significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day, p.o., X 14) showed a significant healing effect, which was higher than that of propantheline bromide. BTM-1086 at a dose of 0.2 mg/kg, i.d., remarkably inhibited the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K+ as well as the increments of the volume and Na+ in the gastric secretion were prevented dose-dependently by pretreatment with BTM-1086. 相似文献
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Ferry Verbaan Inger van Dam Yoshinubu Takakura Mitsuru Hashida Wim Hennink Gert Storm Christien Oussoren 《European journal of pharmaceutical sciences》2003,20(4-5):419-427
The objective of this study was to assess the in vivo fate of poly(2-(dimethylamino)ethyl methacrylate) (pDMAEMA)-based polyplexes after intravenous administration into mice. Circulation kinetics and tissue distribution in terms of plasmid localization and transfection efficiency were assessed. To gain more insight into the observed biodistribution and gene expression profile, the interaction of pDMAEMA-based polyplexes with blood components (erythrocytes and albumin) was investigated in vitro. In the case of i.v. injection of positively charged polyplexes at a dose of 30 microg DNA most of the radioactivity was found in the lungs and the liver 60 min after injection. In the case of pDMAEMA/DNA polyplexes with a negative charge, uptake occurred mainly by the liver. Administration of positively charged complexes at a 30 microg DNA dose resulted in reporter gene expression primarily in the lungs. Injection of negatively charged complexes and naked plasmid did not result in luciferase expression in any of the organs examined. In vitro turbidity experiments showed the induction of a charge dependent aggregation process upon addition of albumin to the polyplexes pointing out to the involvement of aggregate formation in the dominant lung uptake of the positively charged polyplexes. Also, incubations of polyplexes after pre-incubation with a physiological concentration of albumin with washed erythrocytes confirmed that polyplexes induce the formation of extremely large structures. This paper underlines the need for the design of systems with reduced interaction with blood components to promote the delivery of DNA to target tissues outside the lungs. 相似文献
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Archives of Pharmacal Research - Penicillin G potassium salt was transformed in high yield to 4-acetoxy-3-phenylacetaminoazetidinone by treatment of mercury acetate, ozonolysis and methanol in... 相似文献
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Preparation of 2,3-dihydro-1,3,2-benzoxazaphosphorin-4-one derivatives and their 2-oxo derivatives is described. Compounds 1 and 12 have anticancer activity. 相似文献
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Croston GE Olsson R Currier EA Burstein ES Weiner D Nash N Severance D Allenmark SG Thunberg L Ma JN Mohell N O'Dowd B Brann MR Hacksell U 《Journal of medicinal chemistry》2002,45(23):4950-4953
A functional cell-based screen identified 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one hydrochloride (AC-7954, 1) as a nonpeptidic agonist of the urotensin-II receptor. Racemic 1 had an EC50 of 300 nM at the human UII receptor and was highly selective. Testing of the enantiopure (+)- and (-)- 1 revealed that the UII receptor activity of racemic 1 resides primarily in (+)-1. Being a selective nonpeptidic druglike UII receptor agonist, (+)-1 will be useful as a pharmacological research tool and a potential drug lead. 相似文献
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丙酰肼与三光气缩合环化得到5-乙基-1,3,4-噁二唑-2(3H)-酮,继与2-苯氧乙胺反应后在碱性条件下环合得到抗抑郁药奈法唑酮中间体5-乙基-2,4-二氢-4-(2-苯氧乙基)-3H-1,2,4-三唑-3-酮,总收率66.3%. 相似文献
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A group of 20 female neurotic inpatients has been treated with 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one-(chlordesmethyldiazepan)- 7-chloro-5(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one (lorazepam) according to a double-blind cross-over design. For each drug clinical evaluations were performed by means of Hamilton's rating scale for anxiety states and of Overall and Gorham's brief psychiatric rating scale, at the beginning, after the first week and at the end of the two-week period of treatment, in opposite sequence. A statistically greater efficacy of chlordesmethyldiazepam in comparison to lorazepam was observed. Results are discussed with regard to benzodiazepine structure-activity relationships. 相似文献
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