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  • Title: In vitro and in vivo comparisons of antiandrogenic potencies of two histamine H2-receptor antagonists, cimetidine and etintidine--HCl.
    Author: Foldesy RG, Vanderhoof MM, Hahn DW.
    Journal: Proc Soc Exp Biol Med; 1985 Jun; 179(2):206-10. PubMed ID: 2859600.
    Abstract:
    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 vitro and 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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