Abstract
Summary
Betahistine and demethylbetahistine lower arterial blood pressure in the rat, and the depressor response was blocked by pretreatment with the antihistamine, tripelennamine. Rats pretreated with SKF-525-A exhibited no modification of the depressor action of betahistine. No detectable betahistine N-demethylase activity was observed in rat liver homogenates. The data do not support the contention that demethylbetahistine contributes to the overall depressor response observed after intravenous administration of betahistine, and suggest that direct deamination of betahistine may represent the major pathway of enzymatic degradation of this drug in the rat.
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