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新型镇咳药左羟丙哌嗪的一般药理学

General pharmacology of the new antitussive levodropropizine.

作者信息

Melillo G, Malandrino S, Rossoni G, Caselli G, Bestetti A, Borsa M, Tonon G C, Berti F

机构信息

Research & Development Laboratories, Dompé Farmaceutici S.p.A., Milan, Italy.

出版信息

Arzneimittelforschung. 1988 Aug;38(8):1144-50.

PMID:3196408
Abstract

The general pharmacological profile of levodropropizine (S(-)3-(4-phenyl-piperazin-1-yl)-propane-1,2-diol, DF 526), a new antitussive drug, was compared with that of dropropizine racemate. Levodropropizine had weaker central sedative effects than the racemate and it did not induce physical dependence in rats. When given intravenously or intraperitoneally, levodropropizine did not exert any significant effects on the cardiovascular and respiratory systems. Receptor binding data excluded interaction with beta-adrenergic, muscarinic and opiate receptors. On the contrary, levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors. The affinity was also confirmed with isolated organ preparations. On the basis of this study, levodropropizine appears to have a better tolerability index than the racemate.

摘要

将新型止咳药左羟丙哌嗪(S(-)3-(4-苯基-哌嗪-1-基)-丙烷-1,2-二醇,DF 526)的一般药理学特性与消旋羟丙哌嗪进行了比较。左羟丙哌嗪的中枢镇静作用比消旋体弱,且在大鼠中不产生身体依赖性。静脉内或腹腔内给药时,左羟丙哌嗪对心血管和呼吸系统无任何显著影响。受体结合数据排除了与β-肾上腺素能、毒蕈碱和阿片受体的相互作用。相反,左羟丙哌嗪对H1-组胺能和α-肾上腺素能受体具有亲和力。这种亲和力也在离体器官制剂中得到证实。基于这项研究,左羟丙哌嗪似乎比消旋体具有更好的耐受性指标。

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