氟哌噻吨和舒必利异构体对肾血管中多巴胺受体的阻断作用。

Blockade of dopamine receptors in the renal vasculature by isomers of flupenthixol and sulpiride.

作者信息

Schmidt M, Imbs J L, Giesen E M, Schwartz J

出版信息

J Cardiovasc Pharmacol. 1983 Jan-Feb;5(1):86-9. doi: 10.1097/00005344-198301000-00013.

DOI:10.1097/00005344-198301000-00013

Abstract

We studied the renal vascular effects of flupenthixol and sulpiride isomers in the isolated perfused rat kidney in the presence of phenoxybenzamine (10(-5) M) and sotalol (10(-5) M). The vascular bed was contracted with prostaglandin F2 alpha (10(-7) -3 X 10(-6) M) and dose-dependently relaxed with dopamine. Cis-flupenthixol (10(-9)-10(-7) M) antagonized competitively the response to dopamine (apparent pA2 = 8.34 +/- 0.09; mean +/- SD) without affecting papaverine-induced relaxation. Trans-flupenthixol was without effect at 10(-7) M. The dopamine receptor antagonist activities of the sulpiride isomers are low and d-sulpiride is twice as active as 1-sulpiride. Thus, the renal vascular dopamine receptor can be further characterized by the relative antagonist activities of cis-flupenthixol and sulpiride and by a rather low stereospecificity in favor of d-sulpiride.

摘要

我们在苯氧苄胺（10⁻⁵M）和索他洛尔（10⁻⁵M）存在的情况下，研究了氟哌噻吨和顺式及反式舒必利异构体对离体灌注大鼠肾脏的肾血管作用。血管床用前列腺素F2α（10⁻⁷ - 3×10⁻⁶M）收缩，并用多巴胺剂量依赖性舒张。顺式氟哌噻吨（10⁻⁹ - 10⁻⁷M）竞争性拮抗对多巴胺的反应（表观pA2 = 8.34±0.09；平均值±标准差），而不影响罂粟碱诱导的舒张。反式氟哌噻吨在10⁻⁷M时无作用。舒必利异构体的多巴胺受体拮抗活性较低，d-舒必利的活性是l-舒必利的两倍。因此，肾血管多巴胺受体可以通过顺式氟哌噻吨和舒必利的相对拮抗活性以及有利于d-舒必利的相当低的立体特异性来进一步表征。