Selective Modulation of the ATP-sensitive K+ Channel by Nicorandil in Guinea-pig Cardiac Cell Membrane

Overview

Journal Naunyn Schmiedebergs Arch Pharmacol

Specialty Pharmacology

Date 1990 Nov 1

PMID 2151053

Citations 8

Authors

M Takano

A Noma

Affiliations

Soon will be listed here.

Abstract

Effects of a vasodilator, nicorandil (2-nicotinamidoethyl nitrate) on four kinds for cardiac K+ channels were investigated in guinea pig ventricular and atrial cells using inside-out patch recording combined with "oil-gate" concentration jump method. Nicorandil of 300 mumols/l failed to affect the inward-rectifier K+ channel and the Na(+)-activated K+ channel. The open probability of the muscarinic K+ channel, when activated by the application of GTP, was not changed by the drug. Nicorandil selectively increased the open probability of the ATP-sensitive K+ channel that was partly suppressed by intracellular ATP. The median effective concentration (EC50) of nicorandil was 74 mumols/l and Hill coefficient was 1.32 in the concentration-open probability relationship. The closing rate of the K+ channel by ATP was markedly delayed by the drug, whereas the open rate on removal of ATP was scarcely affected. Nicorandil had only little effect on this channel after run-down. It was concluded that nicorandil selectively activates the ATP-sensitive K+ channel mainly by modulating the ATP-dependent gate.

Citing Articles

Effects of acidosis and NO on nicorandil-activated K(ATP) channels in guinea-pig ventricular myocytes.

Moncada G, Kishi Y, Numano F, Hiraoka M, Sawanobori T Br J Pharmacol. 2000; 131(6):1097-104.

PMID: 11082116 PMC: 1572434. DOI: 10.1038/sj.bjp.0703678.

K channel openers activate different K channels in vascular smooth muscle cells.

Kitamura K, Kamouchi M Cardiovasc Drugs Ther. 1993; 7 Suppl 3:539-46.

PMID: 8251424 DOI: 10.1007/BF00877619.

Mechanism of action of a K+ channel activator BRL 38227 on ATP-sensitive K+ channels in mouse skeletal muscle fibres.

Hussain M, Wareham A, Head S J Physiol. 1994; 478 Pt 3:523-32.

PMID: 7965862 PMC: 1155672. DOI: 10.1113/jphysiol.1994.sp020271.

Time-dependent fading of the activation of KATP channels, induced by aprikalim and nucleotides, in excised membrane patches from cardiac myocytes.

Thuringer D, Cavero I, CORABOEUF E Br J Pharmacol. 1995; 115(1):117-27.

PMID: 7647966 PMC: 1908735. DOI: 10.1111/j.1476-5381.1995.tb16328.x.

Antiischemic effects of nicorandil during coronary angioplasty in humans.

Saito S, Mizumura T, Takayama T, Honye J, Fukui T, Kamata T Cardiovasc Drugs Ther. 1995; 9 Suppl 2:257-63.

PMID: 7647030 DOI: 10.1007/BF00878473.

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