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BAY P 1455,一种在大鼠中具有胃保护特性的噻唑基氨基苯并咪唑衍生物。

BAY P 1455, a thiazolylaminobenzimidazole derivative with gastroprotective properties in the rat.

作者信息

Grassi A, Ippen J, Bruno M, Thomas G

机构信息

Department of Pharmacology, Bayer Italia, Garbagnate M.se MI.

出版信息

Eur J Pharmacol. 1991 Mar 26;195(2):251-9. doi: 10.1016/0014-2999(91)90543-y.

Abstract

The antiulcer activity of BAY P 14551 a thiazolylaminobenzimidazole derivative, was evaluated in different experimental ulcer models and its antiulcer activity was compared to that of different reference drugs. The overall activity of the compound was equal to or more potent than that of reference antiulcer drugs, such as pirenzepine, cimetidine and carbenoxolone, but it was not as potent as rioprostil. The ED50 values (expressed as mumol/kg p.o.) were 68 (confidence limits: 51-91) for indomethacin-induced ulcers, 21 (confidence limits: 13-31) for stress-induced ulcers and 1260 mumol/kg p.o. (confidence limits: 412-3800) for ulcers induced by absolute ethanol. The compound had no activity against cysteamine-induced duodenal ulcers and lost its cytoprotective activity in adrenalectomised rats. Since inhibition of gastric acid secretion was seen, if at all, only with the higher doses, the gastro-protective action of BAY P 1455 seemed not to be due to an antisecretory effect, but more likely to a gastroprotective action as hypothesised for prostaglandins.

摘要

噻唑基氨基苯并咪唑衍生物BAY P 14551的抗溃疡活性在不同的实验性溃疡模型中进行了评估,并将其抗溃疡活性与不同的参比药物进行了比较。该化合物的总体活性等于或强于参比抗溃疡药物,如哌仑西平、西咪替丁和甘珀酸,但不如瑞前列醇强效。吲哚美辛诱导的溃疡的ED50值(以μmol/kg口服表示)为68(置信限:51 - 91),应激诱导的溃疡为21(置信限:13 - 31),无水乙醇诱导的溃疡为1260 μmol/kg口服(置信限:412 - 3800)。该化合物对半胱胺诱导的十二指肠溃疡无活性,且在肾上腺切除的大鼠中失去了其细胞保护活性。由于仅在较高剂量下才观察到胃酸分泌的抑制,BAY P 1455的胃保护作用似乎不是由于抗分泌作用,而更可能是如对前列腺素所假设的胃保护作用。

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