COMPARATIVE-STUDY OF THE RAT UTERINE SMOOTH-MUSCLE RELAXANT ACTIVITY OF 3 BISBENZYLTETRAHYDROISOQUINOLINES WITH TETRANDRINE

被引:9
作者
ZAFRAPOLO, MC
TORMOS, MJ
CORTES, D
ANSELMI, E
机构
[1] Laboratorio de Farmacognosia y Farmacodinamia, Departamento de Farmacología, Facultad de Farmacia, Universidad de Valencia
关键词
D O I
10.1111/j.2042-7158.1993.tb05599.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The relaxant activity of three bisbenzyltetrahydroisoquibolines-obaberine popisonine and lindoldhamine-was examined in rat isolated uterus and their inhibitory potencies were compared with that of tetrandrine. All alkaloids tested relaxed KCl-depolarized rat uterus and totally or partially inhibited oxytocin-induced rhythmic contractions. The degree of methylation of the free phenolic hydroxy groups and the loss of one diarylether bridge influence the potency of relaxant action of these alkaloids. Only alkaloids with absolute configuration 1R,1'S or 1R1'R acted intracellularly, promoting relaxation of contractile responses induced by oxytocin or vanadate in a Ca2+-free MediUM.
引用
收藏
页码:563 / 566
页数:4
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