促黄体生成素释放激素类似物对促黄体生成素释放及排卵的拮抗作用。
Antagonism of luteinizing hormone release and of ovulation by an analog of the luteinizing hormone-releasing hormone.
作者信息
Yardley J P, Foell T J, Beattie C W, Grant N H
出版信息
J Med Chem. 1975 Dec;18(12):1244-7. doi: 10.1021/jm00246a015.
PMID:1104833
Abstract
Two varients of LH-RH, less than Glu-D-Phe-Trp-D-Ala-Leu-Arg-Pro-Gly-NH2 (I) and less than Glu-D-Phe-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-NHCH2CH3 (II), have been synthesized by solid-phase methods. Both peptides strongly inhibit the LH-RH induced secretion of LH in an in vitro assay; however, only I proved effective in preventing ovulation in the 4-day cycling rat.
摘要
已通过固相法合成了两种促黄体生成激素释放激素（LH-RH）变体，它们比谷氨酸-对氟苯丙氨酸-色氨酸-天冬氨酸-丙氨酸-亮氨酸-精氨酸-脯氨酸-甘氨酰胺（I）短，且比谷氨酸-对氟苯丙氨酸-色氨酸-丝氨酸-酪氨酸-天冬氨酸-亮氨酸-精氨酸-脯氨酰胺基乙烷（II）短。在体外试验中，这两种肽均强烈抑制LH-RH诱导的促黄体生成激素（LH）分泌；然而，只有I在4日周期的大鼠中被证明对防止排卵有效。
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