PMID: 41059Sep 1, 1979

Non-competitive-non-equilibrium alpha-adrenoceptor blocking properties of N-benzyl iodoacetamide, betsamide

The Journal of Pharmacy and Pharmacology
J P Huidobro-ToroH Miranda

Abstract

N-Benzyl iodoacetamide, betsamide, at 10 mg kg-1 i.v. blocked the hypertensive and contractile responses of the nictitating membrane of the cat to adrenaline. The blockade had a lag period before full development. Pretreatment of cats with betsamide for 7 or 18 h showed a non-equilibrium type of alpha-adrenoceptor blockade. The responses of the nictitating membrane to adrenaline were markedly depressed and did not recover after high doses of adrenaline. In the same cats, adrenaline caused a profound hypotension. The effect of betsamide lasted for at least 72 h. In the rat isolated vas deferens, 3 X 10(-5) M betsamide non-competitively blocked the contractile responses to noradrenaline; the adrenoceptor blockade was less effective when betsamide was applied with noradrenaline. The blockade lasted for more than 24 h, and was not reversible after extensive washing. Betsamide antagonized the contractile effects of carbachol and 5-hydroxytryptamine on the rat vas deferens, but not the beta-responses of the guinea-pig trachea to adrenaline and isoproenaline. Results are discussed in relation to a probable mechanism of action.

Citations

Nov 11, 2005·Archiv der Pharmazie·José Marco-Contelles, Elena Gómez-Sánchez

Related Concepts

Adrenergic alpha-Antagonists
Felis catus
Medihaler-Epi
Hemodynamics
Iodoacetamide
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Smooth Muscle
Trachea
Vas Deferens Structure

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