In Vitroand in VivoComparisons of Antiandrogenic Potencies of Two Histamine H2-Receptor Antagonists, Cimetidine and Etintidine-HCI

Autor: Foldesy, Robin G., Vanderhoof, Mary M., Hahn, Do Won
Zdroj: Experimental Biology and Medicine; June 1985, Vol. 179 Issue: 2 p206-210, 5p
Abstrakt: The antiandrogenic potency of cimetidine was compared to that of a new histamine H2-receptor antagonist, etintidine-HCl (ORF 16753-02). Although both compounds displaced [3H]dihydrotestosterone from androgen receptors in vitroand inhibited androgen-stimulated growth of the accessory sex organs of male rats in vivo, etintidine-HCl was significantly less antiandrogenic than cimetidine in the analysis of androgen receptor binding and in the inhibition of seminal vesicle weights. Because etintidine-HCl has been shown previously to have more potent gastric antisecretory activity than cimetidine, its lower antiandrogenic activity suggests that etintidine-HCl has a much wider therapeutic ratio and that its use clinically will result in fewer antiandrogenic side effects.
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