犬胃黏膜细胞中对组胺H2受体兴奋敏感的腺苷酸环化酶系统的特性研究
Characterization of an adenylate cyclase system sensitive to histamine H2-receptor excitation in cells from dog gastric mucosa.
作者信息
Scholes P, Cooper A, Jones D, Major J, Walters M, Wilde C
出版信息
Agents Actions. 1976 Nov;6(6):677-82. doi: 10.1007/BF02026087.
PMID:188329
Abstract
A method of preparing viable cells from dog gastric mucosa is described. Cyclic AMP in these cells is elevated by histamine and 4-methyl histamine but 2-methyl histamine is only a weak agonist. The effects on cyclic AMP levels are inhibited competitively by metiamide and burimamide which give apparent KBvalues of 3.5x10-7 M and 2.3x10-6 M, respectively. These values are similar to those reported for other histamine H2-receptor systems. The H1-receptor antagonists, mepyramine and chlorpheniramine, have no inhibitory effect on the histamine induced elevation of cyclic AMP: promethazine inhibits the system but not by a competitive mechanism. It is concluded that the histamine stimulated adenylate cyclase system is probably located in the parietal cell component.
摘要
本文描述了一种从犬胃黏膜制备活细胞的方法。组胺和4-甲基组胺可使这些细胞中的环磷酸腺苷（cAMP）水平升高，但2-甲基组胺只是一种弱激动剂。甲硫米特和布立马胺可竞争性抑制对cAMP水平的影响，其表观解离常数（KB）分别为3.5×10-7M和2.3×10-6M。这些值与其他组胺H2受体系统报道的值相似。H1受体拮抗剂美吡拉敏和氯苯那敏对组胺诱导的cAMP升高无抑制作用：异丙嗪可抑制该系统，但不是通过竞争机制。得出的结论是，组胺刺激的腺苷酸环化酶系统可能位于壁细胞成分中。
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