BOMT (6 alpha-bromo-17 beta-hydroxy-17 alpha-methyl-4-oxa-5 alpha-androstan-3-one) is not an androgen antagonist within the central nervous system.
This study investigates the efficiency of BOMT as an androgen antagonist within the central nervous system. The efficiency of BOMT in suppressing neural receptor binding of testosterone, and the ability of this antiandrogen to block the feedback loop of testosterone onto the central nervous system, as evidenced by plasma testosterone levels, is reported. BOMT was found to be unable to open the feedback loop of testosterone onto the central nervous system, which was correlated with the low competing efficiency of this antiandrogen for receptor sites in vitro within the hypothalamic-preoptic area of the brain - a region known to be involved in gonadotrophin secretion. The observed divergence in the degree of antiandrogenicity of BOMT between peripheral and central target tissues of testosterone is discussed.
D000726:Androgen Antagonists / Q000494:pharmacology*; D000731:Androstanes / Q000494:pharmacology*; D000818:Animals; D002369:Castration; D003429:Cross Reactions; D007031:Hypothalamus / Q000378:metabolism; D008297:Male; D051379:Mice; D009929:Organ Size; D011467:Prostate / Q000187:drug effects; D011863:Radioimmunoassay; D011944:Receptors, Androgen / Q000187:drug effects*; D011987:Receptors, Steroid / Q000187:drug effects*; D013257:Steroids, Brominated / Q000494:pharmacology; D013260:Steroids, Heterocyclic / Q000494:pharmacology; D013739:Testosterone / Q000037:antagonists & inhibitors / Q000097:blood
D000726:Androgen Antagonists; D000731:Androstanes; D011944:Receptors, Androgen; D011987:Receptors, Steroid; D013257:Steroids, Brominated; D013260:Steroids, Heterocyclic; D013739:Testosterone