Influence of Calcium Entry Blockers and Calmodulin Inhibitors on 5-Hydroxytryptamine-, Potassium- and Calcium-induced Contractions in Human Umbilical Artery In-vitro

Author:

Medeiros Yara S1,Calixto João B1

Affiliation:

1. Department of Pharmacology, CCB, Universidade Federal de Santa Catarina, 88015 Florianópolis, SC, Brazil

Abstract

Abstract The effects of calcium (Ca2+) withdrawal, Ca2+ entry blockers and calmodulin inhibitors on the contractile responses to 5-hydroxytryptamine (5-HT), K+ and CaCl2 have been studied in human isolated umbilical artery. Following Ca2+ withdrawal from the medium (30 min), both 5-HT- and K+ -induced contractions were virtually abolished. Ca2+ entry blockers (nifedipine, verapamil, diltiazem and cinnarizine) were significantly more effective in inhibiting 5-HT- than K+-induced contractions. In relation to calmodulin inhibitors, trifluoperazine inhibited all types of contractions, whereas W-7 (N-6-aminohexyl-5-chloro-1-naphthalene sulphonamide) only inhibited 5-HT- and CaCl2-induced contractions. All drugs inhibited CaCl2-induced contractions in a non-competitive manner. These findings indicate that the mechanisms by which these drugs exert their inhibitory effects on human umbilical artery are markedly different from those reported in other vascular beds.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Reference25 articles.

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2. Pharmacological properties of N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7), a calmodulin antagonist in arterial strips from rats and rabbits;Asano;J. Pharmacol. Exp. Ther.,1985

3. In vitro effects of calcium entry blockers, chlorpromazine and fenoterol upon human pregnant myometrium contractility;Ballejo;Br. J. Pharmacol.,1986

4. 5-Hydroxy-tryptamine receptors in human umbilical artery: functional and binding studies;Brown;Br. J. Pharmacol.,1987

5. Effect of diphenylhydantoin on drug and calcium-induced contractions of isolated rat uterus. A comparative study with nifedipine;Calixto;Gen. Pharmacol.,1987

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