Comparison of the potential for therapeutic utilities with gonadotropin-releasing hormone agonists and antagonists.

作者: BRIAN H. VICKERY

DOI: 10.1210/EDRV-7-1-115

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摘要: Introduction THE SUCCESS in synthesis of very potent agonistic analogs GnRH was at first expected to lead a low cost profertility therapy. Early findings gonadal suppressive effects with these agents, however, led the discovery pituitary receptor desensitization and downregulation caused by continuous presence its analogs. It then established that must be secreted pulsatile manner exert physiological effect activating reproductive cascade from gonadotropin release steroidogenesis gametogenesis. Only after application this knowledge has become valuable therapeutic agent hypogonadotropic hypogonadism (1). A number highly have now been described are various stages clinical evaluation (see Table 1). The increases potency over native hormone related increased binding affinity consequent retardation dissociation rate receptors (3). In addition, some analog...

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