定义的组胺H2-receptor大脑:LSD的交互。
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绿色的摩根大通,温斯坦H, Maayani年代
定义的组胺H2-receptor大脑:LSD的交互。
尼达Res Monogr。1978; (22): 38-59。
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30911年(在PubMed]
- 文摘
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两个方面的药物的作用方式的复杂性。一个是定义的标准和陷阱与特定的受体相互作用。另一个是需要考虑每一种药物的药理作用受体连接的事件,因为它变得清楚,每种药物可能有相当大的许多特定受体亲和力。说明这些想法是组胺受体的特性与腺苷酸环化酶在大脑。一系列的活动H2-antagonists和H2-agaonists被证明是相同的组胺受体与腺苷酸环化酶在已知H2-receptors。受体激动剂的KB的拮抗剂和ED50值值没有区分这些受体之一。值得注意的是,在高浓度时,H2-receptor H1-antagonists也是竞争对手。赛庚啶H2-receptor尤其是高亲和力。这是最有效的H2-antagonist尚未报道。其他出版结果综述了展示赛庚啶的各种受体的亲和力。 Its affinity for serotonin receptors led us to examine other serotonin antagonists. On this H2-receptor linked to adenylate cyclase in homogenates of guinea pig hippocampus and cortex, D-LSD and D-2-bromo-LSD (BrLSD) were shown to be competitive antagonists of histamine. L-LSD, mescaline and psilocin were inactive. Noting congurency in the molecular structyre of D-LSD and known H2-antagonists, we predicted a new H2-antagonist. This prediction is shown to be correct: the compound has similar affinity to the H2-receptor as has LSD. The affinities of D-LSD and BrLSD for the H2-receptor are compared with their affinities for other receptors. The pharmacology of D-LSD and BrLSD is reviewed. Evidence is assembled that BrLSD has considerable central effects.