Bethanidine increases one type of potassium current and relaxes aortic muscle.

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Bkaily G, Caille JP, Payet MD, Peyrow M, Sauve R, Renaud JF, Sperelakis N

Bethanidine increases one type of potassium current and relaxes aortic muscle.

Can J Physiol Pharmacol. 1988 Jun;66(6):731-6.

PubMed ID

3167688 [ View in PubMed

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Abstract

Using a whole-cell voltage-clamp technique, we identified two time- and voltage-dependent K+ currents: an early outward rectifier and a delayed outward rectifier in single vascular smooth muscle cells of rabbit aorta in culture. About 90% of the single cells tested showed a predominant delayed outward K+ current type. Both K+ currents were decreased by tetraethylammonium. In contrast, bethanidine sulphate (10(-4)M), a pharmacological analog of the cardiac antifibrillatory drug, bretylium tosylate, decreased the early outward K+ current, increased the delayed rectifier K+ current type, and hyperpolarized the resting membrane potential. Bethanidine was found to relax vascular smooth muscle. The vasodilatory effect of bethanidine is associated with the activation of a K+ current that is probably involved in keeping the membrane potential at the resting state, thereby depressing the excitability of the aortic vascular smooth muscle.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Bethanidine	ATP-sensitive inward rectifier potassium channel 1	Protein	Humans	Yes	Inhibitor	Details