Clark C R, Nowell N W
Steroids. 1979 Aug;34(2):139-49. doi: 10.1016/0039-128x(79)90043-6.
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.
本研究调查了BOMT作为中枢神经系统内雄激素拮抗剂的效能。报告了BOMT在抑制睾酮与神经受体结合方面的效能，以及这种抗雄激素通过血浆睾酮水平所证明的阻断睾酮对中枢神经系统反馈回路的能力。研究发现，BOMT无法打开睾酮对中枢神经系统的反馈回路，这与该抗雄激素在体外对大脑下丘脑-视前区（已知参与促性腺激素分泌的区域）受体位点的低竞争效能相关。文中讨论了在睾酮的外周和中枢靶组织中观察到的BOMT抗雄激素性程度的差异。
