Relaxant Effect of Tetrazepam on Rat Uterine Smooth Muscle: Role of Calcium Movement

Author:

Perez-Guerrero C1,Herrera M D1,Marhuenda E1

Affiliation:

1. Departamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, Sevilla, España

Abstract

Abstract Tetrazepam is a benzodiazepine derivative clinically used as a muscle relaxant. The aim of the present work was to examine its effect on uterine smooth muscle of the rat in estrus. Tetrazepam required micromolar concentractions to relax contractile responses induced by KCl and acetylcholine in Ca2+ solution, but not oxytocin-induced contraction. In Ca2+-free solution, tetrazepam inhibited Ca2+-induced contractions in depolarized uterus and vanadate-induced contractions. We suggest that tetrazepam relaxes contractile responses induced by activation of voltage-sensitive calcium channels and receptor-operated calcium channels with little selectivity or that it antagonizes the effect of calcium at subsequent steps, possibly intracellular stores sensitive to vanadate but not sensitive to oxytocin. The inhibition of contraction of rat uterus is not related to high-affinity peripheral benzodiazepine binding sites.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Reference30 articles.

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3. Pharmacological evidence that the nonneuronal diazepam binding sites in primary cultures of glial cells is associated with a calcium channels;Bender;Eur. J. Pharmacol.,1985

4. Mechanisms of action of transmitters and other substances on smooth muscle;Bolton;Phisyol. Rev.,1979

5. Role of stored Ca in contractions of rat uterus induced by acetylcholine: effects of preincubation with Mg-free solution;D'Ocón;Arch. Int. Pharmacodyn. Ther.,1987

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