Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency.
Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency.
复制标题
抗精神病药对脑多巴胺、血清素、α-肾上腺素能和组胺受体的作用与临床效力的关系。
DOI：
10.1176/ajp.137.12.1518
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发表时间：
1980
期刊：
影响因子：
--
通讯作者：
Synder,SH
中科院分区：
文献类型：
--
作者：
Peroutka,SJ;Synder,SH
作者研究了22种神经安定药物竞争与多巴胺、5-羟色胺、α-肾上腺素能和组胺受体相关的结合位点的效力。他们发现，尽管许多精神抑制剂在竞争这些受体位点中的几个时相当有效，但抗精神病药物的平均临床效力仅与药物对3 H-螺哌啶标记的多巴胺受体的亲和力密切相关。然而，在临床有效剂量下，经常发生血清素、α-肾上腺素能和组胺受体的大量占用，这可能是精神抑制剂的一些辅助作用的原因。
The authors examined the potencies of 22 neuroleptic drugs competing for binding sites associated with dopamine, serotonin, alpha-adrenergic, and histamine receptors in brain membranes. They found that although many neuroleptics are quite potent in competing at several of these receptor sites, the average antipsychotic clinical potency correlates closely only with the drug affinity for dopamine receptors labeled by 3H-spiroperidol At clinically effective doses, however, substantial occupancy of serotonin, alpha-adrenergic, and histamine receptors often occurs and may account for some of the auxiliary actions of neuroleptics.