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舒必利:去甲肾上腺素和5-羟色胺的弱拮抗剂。

Sulpiride: a weak antagonist of norepinephrine and 5-hydroxytryptamine.

作者信息

Kohli J D, Cripe L D

出版信息

Eur J Pharmacol. 1979 Jun 15;56(3):283-6. doi: 10.1016/0014-2999(79)90185-7.

DOI:10.1016/0014-2999(79)90185-7
PMID:477724
Abstract

Antagonism of norepinephrine (NE) and 5-hydroxytryptamine (5-HT) by sulpiride was studied in vitro on rabbit aortic strips. Concentrations of sulpiride ranging from 3 X 10(-5) to 3 X 10(-3) M caused a progressive shift of the dose response curves of both NE and 5-HT to the right without inhibiting the responses to KCl. pA2 values of sulpiride calculated from Schild plots against NE and 5-HT were 4.6 and 4.4, respectively. Thus, sulpiride, which has been previously shown to be the most potent antagonist of the dopamine vascular receptors, is a very weak alpha-adrenergic or 5-HT antagonist.

摘要

在体外对兔主动脉条研究了舒必利对去甲肾上腺素(NE)和5-羟色胺(5-HT)的拮抗作用。舒必利浓度范围为3×10⁻⁵至3×10⁻³M时,可使NE和5-HT的剂量反应曲线逐渐右移,而不抑制对氯化钾的反应。根据Schild图计算出的舒必利对NE和5-HT的pA2值分别为4.6和4.4。因此,舒必利先前已被证明是多巴胺血管受体的最有效拮抗剂,却是一种非常弱的α-肾上腺素能或5-HT拮抗剂。

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