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1971年下丘脑LHRH(即促黄体生成素释放激素)结构的阐明和人工合成,明确了中枢神经系统对垂体的控制作用,大大推动了神经内分泌学和生殖生理学的发展。为了寻找非甾体避孕药,人们利用同一时期发展起来的固相肽合成技术,合成了两千余LHRH类似物,其中大部份是拮抗类似物(以下简称拮抗剂)。虽然LHRH拮抗剂的研究几乎与激动剂的研究同时起步,但经历了复杂得多的过程后才得到了超高活性的拮抗剂。LHRH拮抗剂与激动剂的作用机理不同,很有希望成为更易于接受的新型非甾体避孕药。本文对其抗生育研究进展做一概述。
1971 Hypothalamus LHRH (ie, luteinizing hormone releasing hormone) structure elucidation and artificial synthesis of the central nervous system to clarify the role of the pituitary gland, greatly promoted the development of neuroendocrinology and reproductive physiology. In order to find non-steroidal contraceptives, more than two thousand LHRH analogs have been synthesized using solid-phase peptide synthesis developed in the same period, most of which are antagonistic analogs (hereinafter referred to as antagonists). Although studies of LHRH antagonists have started almost simultaneously with agonist studies, they have undergone a much more complex process leading to highly active antagonists. LHRH antagonists and agonists of different mechanisms of action, promising to become more easily accepted new non-steroidal contraceptives. This article gives an overview of its progress in anti-fertility research.