Sandow J
Psychoneuroendocrinology. 1983;8(3):277-97. doi: 10.1016/0306-4530(83)90003-3.
Luteinizing hormone releasing-hormone (LHRH) and its highly active agonists are under clinical investigation for the control of reproductive function and for suppression of hormone dependent tumours. The regulation of LHRH action by pituitary receptors and expression of the biological LHRH effect by gonadotropin release and activation of steroid biosynthesis are discussed in this context. Pituitary LHRH receptors are controlled by autoregulation via endogenous LHRH secretion. The gonadal response to LHRH stimulation is regulated by LH action on receptors for LH, prolactin and FSH. Pituitary and gonadal inhibition are achieved by different mechanisms. Continuous exposure to LHRH blocks gonadotropin release and reduces pituitary LH/FSH content, whereas inhibition of steroid biosynthesis requires daily LH release to maintain receptor down-regulation. Pituitary enzymes involved in LHRH degradation at the receptor site are required for terminating hormone action, but their role in modulating hormonal responsiveness is secondary to receptor regulation. Direct gonadal effects of LHRH are exerted in the presence of gonadotropins by modulating the gonadotropin effect, e.g. in hypophysectomized animals. The presence of specific receptors for LHRH agonists in ovarian and testicular tissue suggests local control mechanisms for gonadotropin activation of steroid biosynthesis.
促黄体生成激素释放激素（LHRH）及其高活性激动剂正在进行临床研究，用于控制生殖功能和抑制激素依赖性肿瘤。本文讨论了垂体受体对LHRH作用的调节以及促性腺激素释放和类固醇生物合成激活对LHRH生物学效应的表达。垂体LHRH受体通过内源性LHRH分泌的自动调节来控制。性腺对LHRH刺激的反应受LH对LH、催乳素和FSH受体的作用调节。垂体和性腺的抑制通过不同机制实现。持续暴露于LHRH会阻断促性腺激素释放并降低垂体LH/FSH含量，而抑制类固醇生物合成则需要每日LH释放以维持受体下调。在受体部位参与LHRH降解的垂体酶是终止激素作用所必需的，但其在调节激素反应性方面的作用仅次于受体调节。LHRH的直接性腺效应是在促性腺激素存在的情况下通过调节促性腺激素效应来发挥的，例如在垂体切除的动物中。卵巢和睾丸组织中存在LHRH激动剂的特异性受体，提示存在促性腺激素激活类固醇生物合成的局部控制机制。
