Interaction of histamine H2-receptor antagonists with GABA and benzodiazepine binding sites in the CNS.

Interaction of histamine H2-receptor antagonists with GABA and benzodiazepine binding sites in the CNS.
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组胺 H2 受体拮抗剂与 CNS 中 GABA 和苯二氮卓结合位点的相互作用。

DOI:
10.1016/0014-2999(83)90011-0
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发表时间:
1983
影响因子:
5
通讯作者:
Gallager,DW
Gallager,DW
中科院分区:
医学2区
文献类型:
--
作者:
Lakoski,JM;Aghajanian,GK;Gallager,DW

文献摘要

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The histamine H2-receptor antagonist cimetidine potently inhibited [3H]muscimol and enhanced [3H]flunitrazepam binding in membranes prepared from several brain regions in the rat, including the dorsal raphe nucleus. As further examined in cortical membranes, this effect on both GABA and benzodiazepine binding sites was specific for imidazole-derived H2-receptor antagonists (potency: cimetidine > metiamide > tiotidine) and not observed with either several H1-receptor antagonists or histamine. These data indicate a striking similarity between the actions of cimetidine (and other imidazole-derived H2-receptor antagonists) and GABA on binding parameters at the GABA receptor complex.