In vitro and in vivo comparisons of antiandrogenic potencies of two histamine H2-receptor antagonists, cimetidine and etintidine--HCl.
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.
Foldesy
R G
RG
Vanderhoof
M M
MM
Hahn
D W
DW
D000726:Androgen Antagonists / Q000494:pharmacology*; D000818:Animals; D002927:Cimetidine / Q000494:pharmacology*; D013196:Dihydrotestosterone / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D007093:Imidazoles / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011944:Receptors, Androgen / Q000187:drug effects
D000726:Androgen Antagonists; D006635:Histamine H2 Antagonists; D007093:Imidazoles; D011944:Receptors, Androgen; D013196:Dihydrotestosterone; D002927:Cimetidine; C036616:etintidine