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INHIBITORS OF EPPIN/SEMENOGELIN BINDING AS MALE CONTRACEPTIVES

机译:EPPIN / SEMENOGELIN抑制剂作为男性避孕药

摘要

Compounds suitable for use in providing male contraception, an assay method for identifying such compounds, and methods of providing contraception using the compounds, are provided. The compounds described herein inhibit Eppin-semenogelin binding, and inhibit forward motility of sperm in humans and other primates. The assays identify compounds which both inhibit eppin-semenogelin binding and inhibit sperm motility, and can be carried out in a high throughput manner, using labeled recombinant Eppin and semenogelin. The compounds can be used in oral or transdermal compositions to temporarily and reversibly inhibit male fertility. They can also be used in addition to, or in place of, spermicides in spermicidal compositions, such as those used in conjunction with condoms, diaphragms, and spermicidal jellies.
机译:提供了适用于提供男性避孕的化合物,用于鉴定此类化合物的测定方法以及使用所述化合物提供避孕的方法。本文所述的化合物抑制Eppin-semenogelin结合,并抑制人和其他灵长类动物的精子向前运动。该测定法鉴定了既抑制eppin-semenogelin结合又抑制精子运动的化合物,并且可以使用标记的重组Eppin和精液凝胶蛋白以高通量方式进行。该化合物可用于口服或经皮组合物中以暂时和可逆地抑制雄性生育。它们也可以作为杀精组合物中的杀精剂的补充或替代,例如与避孕套,隔膜和杀虫胶冻结合使用的杀精剂。

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