TETRANDRINE AND ISOTETRANDRINE, 2 BISBENZYLTETRAHYDROISOQUINOLINE ALKALOIDS FROM MENISPERMACEAE, WITH RAT UTERINE SMOOTH-MUSCLE RELAXANT ACTIVITY

被引:16
作者
DOCON, P
BLAZQUEZ, MA
BERMEJO, A
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.2042-7158.1992.tb05468.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of two bisbenzyltetrahydroisoquinoline alkaloids, 1S, 1'S tetrandrine and its isomer 1R, 1'S isotetrandrine, were investigated in rat isolated uterus in order to identify the mechanism of relaxant action and to study the influence of the absolute configuration on the activity of these alkaloids. Both inhibited the uterine contraction induced by high K+, acetylcholine and oxytocin. In Ca2+-free medium, isotetrandrine relaxed the sustained contraction induced by oxytocin but tetrandrine did not. The relaxant effects of the alkaloids may be due to blockade of calcium influx through specific channels. Tetrandrine and isotetrandrine modify the calcium channel in a nonreversible manner whilst only isotetrandrine acts intracellularly. Tetrandrine shows a more specific relaxant activity as a calcium entry blocker.
引用
收藏
页码:579 / 582
页数:4
相关论文
共 16 条
[1]   SELECTIVE-INHIBITION OF CALCIUM ENTRY INDUCED BY BENZYLISOQUINOLINES IN RAT SMOOTH-MUSCLE [J].
ANSELMI, E ;
FAYOS, G ;
BLASCO, R ;
CANDENAS, L ;
CORTES, D ;
DOCON, P .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1992, 44 (04) :337-343
[2]   A COMPARISON OF UTERINE CONTRACTION INDUCED BY PGE1 AND OXYTOCIN IN CA-FREE SOLUTION [J].
ANSELMI, E ;
DOCON, P ;
VILLAR, A .
PROSTAGLANDINS, 1987, 34 (03) :351-358
[3]   MECHANISMS OF ACTION OF TRANSMITTERS AND OTHER SUBSTANCES ON SMOOTH-MUSCLE [J].
BOLTON, TB .
PHYSIOLOGICAL REVIEWS, 1979, 59 (03) :606-718
[4]   ALKALOIDS OF LIMACIOPSIS-LOANGENSIS [J].
CAVE, A ;
LEBOEUF, M ;
HOCQUEMILLER, R ;
BOUQUET, A ;
FOURNET, A .
PLANTA MEDICA, 1979, 35 (01) :31-41
[5]  
DOCON MP, 1987, ARCH INT PHARMACOD T, V286, P162
[6]  
DOCON MP, 1989, ARCH INT PHARMACOD T, V297, P205
[7]   EFFECTS OF MAGNESIUM-CHLORIDE ON THE CONTRACTILE RESPONSE OF UTERUS TO SEVERAL AGONISTS IN CA-FREE SOLUTION [J].
DOCON, MP ;
ANSELMI, E ;
VILLAR, A .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1987, 39 (06) :444-448
[8]   INHIBITION OF CALCIUM ENTRY INDUCED BY CULARINES AND ISOCRASIFOLINE IN UTERINE SMOOTH-MUSCLE [J].
DOCON, P ;
BLASCO, R ;
CANDENAS, L ;
IVORRA, D ;
LOPEZ, S ;
VILLAVERDE, C ;
CASTEDO, L ;
CORTES, D .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 196 (02) :183-187
[9]   THE SPASMOGENIC ACTION OF OXYTOCIN IN THE RAT UTERUS COMPARISON WITH OTHER AGONISTS [J].
EDWARDS, D ;
GOOD, DM ;
GRANGER, SE ;
HOLLINGSWORTH, M ;
ROBSON, A ;
SMALL, RC ;
WESTON, AH .
BRITISH JOURNAL OF PHARMACOLOGY, 1986, 88 (04) :899-908
[10]  
FANG DC, 1986, CHINESE MED J-PEKING, V99, P638