EFFECTS OF CROMAKALIM ON THE MEMBRANE POTASSIUM PERMEABILITY OF FROG SKELETAL-MUSCLE INVITRO

被引:12
作者
BENTON, DC [1 ]
HAYLETT, DG [1 ]
机构
[1] UNIV LONDON UNIV COLL,DEPT PHARMACOL,GOWER ST,LONDON WC1E 6BT,ENGLAND
基金
英国惠康基金;
关键词
CROMAKALIM; SKELETAL MUSCLE; GLIBENCLAMIDE; POTASSIUM PERMEABILITY;
D O I
10.1111/j.1476-5381.1992.tb14478.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1 The effects of the potassium channel opener, cromakalim, and its active enantiomer, lemakalim, have been investigated in frog skeletal muscle. 2 Cromakalim (30-300-mu-M) increased Rb-86 efflux from muscles loaded with the isotope, hyperpolarized the fibres and reduced membrane resistance. 3 These effects were inhibited by the sulphonylureas, glibenclamide and tolbutamide. The IC50 for glibenclamide inhibition of Rb-86 efflux was ca. 8 nM. 4 Phentolamine (300-mu-m) (which blocks responses to cromakalim in smooth muscle and inhibits ATP-sensitive K+ channels in pancreatic beta-cells) had no effect on the reduction in membrane resistance caused by 100-mu-M lemakalim. 5 Diazoxide (600-mu-M) had no effect on Rb-86 efflux. 6 The similarities of the K+ channel activated by cromakalim in frog skeletal muscle to the channel acted on in smooth muscle and to the ATP-sensitive K+ channel of beta-cells are discussed.
引用
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页码:152 / 155
页数:4
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