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一种强效促黄体生成素释放激素激动剂在大鼠睾丸中的特异性结合。

Specific binding of a potent LHRH agonist in rat testis.

作者信息

Lefebvre F A, Reeves J J, Séguin C, Massicotte J, Labrie F

出版信息

Mol Cell Endocrinol. 1980 Nov;20(2):127-34. doi: 10.1016/0303-7207(80)90076-3.

Abstract

High affinity binding sites for the potent LHRH agonist [125I][D-Ser(TBU)6, des-Gly-NH2(10)]LHRH ethylamide are present in dissociated rat testicular interstitial cells, a preparation rich in Leydig cells. The iodinated LHRH agonist binds to a single class of high affinity sites at a KD value of 0.12 nM and the number of binding sites is approx. 2500 per interstitial cell. A close correlation is observed between the potency of representative LHRH agonist to stimulate LH release in anterior pituitary cells in culture and their affinity for the testicular binding sites. The presence of specific LHRH receptors in an enriched population of Leydig cells suggests that these receptors could play a role, not only in the antifertility effects of LHRH agonists, but also in the physiological control of testicular functions.

摘要

强效促黄体生成素释放激素(LHRH)激动剂[125I][D-丝氨酸(叔丁基)6,去甘氨酰胺(10)]LHRH乙酰胺的高亲和力结合位点存在于解离的大鼠睾丸间质细胞中,该细胞制剂富含睾丸间质细胞。碘化LHRH激动剂以0.12 nM的KD值与一类高亲和力位点结合,结合位点数量约为每个间质细胞2500个。观察到代表性LHRH激动剂在培养的垂体前叶细胞中刺激促黄体生成素(LH)释放的效力与其对睾丸结合位点的亲和力之间存在密切相关性。在富集的睾丸间质细胞群体中存在特异性LHRH受体,这表明这些受体不仅可能在LHRH激动剂的抗生育作用中发挥作用,还可能在睾丸功能的生理控制中发挥作用。

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