TRICYCLIC ANTIDEPRESSANT DRUGS BLOCK HISTAMINE H-2 RECEPTOR IN BRAIN
TRICYCLIC ANTIDEPRESSANT DRUGS BLOCK HISTAMINE H-2 RECEPTOR IN BRAIN
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DOI：
10.1038/269163a0
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发表时间：
1977-01-01
期刊：
影响因子：
64.8
通讯作者：
MAAYANI, S
中科院分区：
文献类型：
--
作者：
GREEN, JP;MAAYANI, S
赛庚啶是与脑内腺苷酸环化酶相连的组胺H2受体的竞争性拮抗剂，这一观察结果提示化学性质相似的三环类抗抑郁药也可能具有这种活性。为了验证这一假设，四个三环抗抑郁药-代表四种不同的结构类型-进行了测试的H2受体连接腺苷酸环化酶在匀浆的豚鼠海马和皮质。二甲双胍和组胺均用作激动剂。二甲双胍对H2受体具有强效活性，对H1受体的活性可忽略不计，即小于组胺的0.0001% 2。
THE observation that cyproheptadine is a competitive antagonist of the histamine H2receptor linked to adenylate cyclase in brain1suggested that the chemically similar tricyclic antidepressant drugs may also have this activity. To test this hypothesis, four tricyclic antidepressants—representing four different structural types—were tested on the H2receptor linked to adenylate cyclase in homogenates of the guinea pig hippocampus and cortex. Both dimaprit and histamine were used as agonists. Dimaprit has potent activity at the H2receptor with negligible activity at the H1receptor, that is, less than 0.0001% of that of histamine2.