Crabo B G, Zimmerman K J, Gustafson B, Holtman M, Koh T J, Graham E F
Int J Fertil. 1975;20(2):87-94.
Daily feeding of 1 mg of alpha-chlorohydrin per kg body weight to boars prevented fertility completely when the ejaculate was used for insemination. The semen charactreated than in untreated boars, but the sperm morphology was otherwise normal. In vitro addition of 5 mg/epididymal contents from the treated boars revealed normal Na+, K+ and glycerylphosphorylcholine concentrations. The movement of sperm cytoplasmic droplets was completed on all spermatozoa more distally in treated than in untreated boars, but the sperm morphology was otherwise normal. In vitro addition of 5 mg/100 ml of alpha-chlorohydrin to ejaculate boar semen completely inhibited and 2.5 mg/100 ml decreased fertility. Removal of the alpha-chlorohydrin prior to insemination partially restored fertility. 14C-alpha-chlorohydrin was shown to be more firmly bound to boar spermatozoa than 14C-carboxyinulin and could not be removed from the spermatozoa with 3 washings. The contraceptive mechanism of the drug is suggested to be alkylation of the sperm membrane by free alpha-chlorohydrin in the epididymis.
每千克体重每日给公猪投喂1毫克α-氯醇,当使用射精精液进行授精时,会完全阻止生育能力。与未处理的公猪相比,处理后的精液特征有所不同,但精子形态正常。在体外向处理过的公猪附睾内容物中添加5毫克/100毫升,显示钠、钾和甘油磷酸胆碱浓度正常。与未处理的公猪相比,处理过的公猪所有精子上的精子细胞质滴移动在更远处完成,但精子形态正常。在体外向公猪射精精液中添加5毫克/100毫升α-氯醇会完全抑制生育能力,添加2.5毫克/100毫升会降低生育能力。在授精前去除α-氯醇可部分恢复生育能力。已表明14C-α-氯醇比14C-羧基菊粉更牢固地结合在公猪精子上,并且经过3次洗涤也无法从精子中去除。该药物的避孕机制被认为是附睾中游离的α-氯醇使精子膜烷基化。