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苯并氮杂䓬类药物SCH 23390在体内可抑制小鼠脑内的3H-NPA结合。

The benzazepine, SCH 23390, inhibits 3H-NPA binding in mouse brain in vivo.

作者信息

Andersen P H, Nielsen E B

出版信息

Acta Pharmacol Toxicol (Copenh). 1986 Oct;59(4):315-8. doi: 10.1111/j.1600-0773.1986.tb00175.x.

Abstract

The fact that SCH 23390, a selective dopamine (DA) D1 antagonist, blocks the effects of D2 agonists suggests a functional coupling of D1 and D2 receptors. Therefore, the binding of SCH 23390 to D2 receptors was investigated in vivo using 3H-N-n-propylnorapomorphine (NPA), a D2 agonist, and 3H-spiperone and 3H-raclopride, both D2 antagonists. SCH 23390 failed to inhibit 3H-spiperone or 3H-raclopride binding; however, SCH 23390 was relatively potent in inhibiting 3H-NPA binding. These results suggest that (some) antidopaminergic effects of SCH 23390 may result from antagonism of a D2 agonist conformation of the D2 receptor.

摘要

选择性多巴胺(DA)D1拮抗剂SCH 23390可阻断D2激动剂的作用,这一事实表明D1和D2受体之间存在功能偶联。因此,使用D2激动剂3H-N-正丙基去甲阿扑吗啡(NPA)以及两种D2拮抗剂3H-螺哌隆和3H-雷氯必利,在体内研究了SCH 23390与D2受体的结合情况。SCH 23390未能抑制3H-螺哌隆或3H-雷氯必利的结合;然而,SCH 23390在抑制3H-NPA结合方面相对有效。这些结果表明,SCH 23390的(某些)抗多巴胺能作用可能源于对D2受体的D2激动剂构象的拮抗作用。

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