NONSTEROIDAL ANDROGENS FOR MALE CONTRACEPTION

描述(改编自《调查员摘要》)：申请人 建议开发一系列非类固醇雄激素受体激动剂 可作为男性避孕药。三个具体目标是 建议。第一种是合成4种类似于 比卡鲁胺(Casodex)是立体化学纯对映体。这个 第二个是表征这些雄激素受体的结合特性 并评估它们的相对激动剂/拮抗剂活性。这个 三是测试最好的两种化合物的生物活性。 以0.1至50毫克/公斤的剂量给雄性小鼠灌胃60天， 每只雄性与三只雌性交配，并评估药物对 生育力和子代结局的质量。

DESCRIPTION (Adapted from the Investigator's Abstract): The applicant proposes to develop a series of non-steroidal androgen receptor agonists which could be used as male contraceptive agents. Three specific aims are proposed. The first is to synthesize 4 chemicals that are analogs of bicalutamide (Casodex) and are stereochemically pure enantiomers. The second is to characterize the androgen receptor binding properties of these compounds and to assess their relative agonist/antagonist activity. The third is to test the biological activity of the best two compounds by treating male mice for 60 days with doses ranging from 0.1 to 50 mg/kg, mating each male to three females, and assessing the drug effects on fertility and quality of progeny outcome.