COMPARISON OF THE INVITRO EFFECTS OF K+ CHANNEL MODULATORS ON DETRUSOR AND PORTAL-VEIN STRIPS FROM GUINEA-PIGS

被引:50
作者
ZOGRAFOS, P [1 ]
LI, JH [1 ]
KAU, ST [1 ]
机构
[1] ICI AMER INC,ICI PHARMACEUT GRP,DEPT PHARMACOL,WILMINGTON,DE 19897
关键词
GUINEA PIG DETRUSOR STRIP; GUINEA PIG PORTAL VEIN STRIP; K+ CHANNEL OPENERS; K+ CHANNEL BLOCKERS; SPONTANEOUS MYOGENIC ACTIVITY; KCL-EVOKED MYOGENIC ACTIVITY;
D O I
10.1159/000139000
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of K+ channel openers and blockers on smooth muscles of vascular and nonvascular origin from guinea pigs have been investigated. Cromakalim, pinacidil, nicorandil and minoxidil sulfate all abolished the spontaneous myogenic activity of the guinea pig portal vein and the KCl-evoked activity of detrusor strips with the same rank order of potency. Whereas both apamin and charybdotoxin stimulated myogenic activity of the detrusor strips, they produced insignificant effects on spontaneously active portal vein strips and failed to antagonize the mechanoinhibitory effects of cromakalim in the two tissues. Glibenclamide, on the other hand, only stimulated the myogenic activity of portal vein strips but antagonized the mechanoinhibitory effects of cromakalim, pinacidil, nicorandil and minoxidil sulfate ln both tissues. Rubidium, at millimolar concentrations, stimulated the myogenic activity, and antagonized the actions of cromakalim in both tissues. The data indicate that there are definite functional dissimilarities as exhibited by the differential response of the two tissues to K+ channel modulators. These findings may be exploited in the design of new drugs with tissue selectivity.
引用
收藏
页码:216 / 230
页数:15
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