AH 22216对离体兔胃细胞中组胺H2受体介导的胃酸分泌具有强效且特异性的阻断作用。

Potent and specific blockade by AH 22216 of histamine-H2-receptor-mediated acid secretion in isolated rabbit gastric cells.

作者信息

Gespach C, Menez I, Emami S

出版信息

Biosci Rep. 1983 Sep;3(9):871-8. doi: 10.1007/BF01133786.

Abstract

AH 22216 is a new histamine-H2-receptor antagonist which possesses a triazole ring. When compared to cimetidine, AH 22216 is about 100 times more potent (Ki = 0.21 x 10(-8) M) in inhibiting histamine-stimulated acid secretion in isolated rabbit gastric cells. These two antihistamines have no effect on carbachol-stimulated acid secretion in the system. The data indicate that AH 22216 interacts directly and specifically on the gastric H2-receptor of the parietal cell and are consistent with the reported pharmacological potencies of AH 22216 and cimetidine on histamine-induced gastric-acid secretion in vivo. AH 22216 could thus be a useful therapeutic agent in patients with peptic ulcers.

摘要

AH 22216是一种新型的具有三唑环的组胺H2受体拮抗剂。与西咪替丁相比，AH 22216在抑制离体兔胃细胞中组胺刺激的胃酸分泌方面的效力约强100倍（Ki = 0.21×10⁻⁸ M）。这两种抗组胺药对该系统中卡巴胆碱刺激的胃酸分泌均无作用。数据表明，AH 22216直接且特异性地作用于壁细胞的胃H2受体，这与报道的AH 22216和西咪替丁在体内对组胺诱导的胃酸分泌的药理效力一致。因此，AH 22216可能是消化性溃疡患者的一种有用治疗药物。