Prolonged suppression of rat testis function by a depot formulation of Zoladex, a GnRH agonist.
Prolonged suppression of rat testis function by a depot formulation of Zoladex, a GnRH agonist.
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Zoladex（一种 GnRH 激动剂）的储库制剂对大鼠睾丸功能的长期抑制。
DOI：
10.1002/j.1939-4640.1989.tb00144.x
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发表时间：
1989
影响因子：
--
通讯作者：
IAN D. Morris
中科院分区：
文献类型：
--
作者：
J. A. Ward;B.J.A. Furr;B. Valcaccia;Brenda Curry;C. W. Bardin;G. Gunsalus;IAN D. Morris
将强效促性腺激素释放激素 (GnRH) 激动剂 Zoladex (D-Ser(But),6 Aza Gly10-GnRH；ICI 118,630；戈舍瑞林) 的缓释制剂每 28 天皮下注射一次（3.6 mg/depot）给雄性大鼠，持续 2-24 周，以确定垂体睾丸功能被抑制的程度以及是否在整个治疗期间维持抑制。给予 Zoladex 导致睾丸、附睾、精囊和前列腺的重量持续减轻。开始治疗后 2 周内，下降明显。观察到生精小管的片状变性和间质细胞萎缩，但没有进展超过治疗1个月后观察到的程度。治疗 2 周后，血清和睾丸睾酮以及睾丸 [125I]hCG 结合显着降低。血清促性腺激素也因治疗而降低。血清雄激素结合蛋白（ABP）升高，睾丸ABP含量不变，附睾ABP含量降低。这些变化与该化合物影响垂体前叶和睾丸的假设一致。这些发现表明，储库递送系统是一种为持续治疗方案施用 GnRH 类似物的便捷方法。
A sustained-release formulation of a potent gonadotropin-releasing hormone (GnRH) agonist, Zoladex (D-Ser(But),6 Aza Gly10-GnRH; ICI 118,630; goserelin), was administered subcutaneously (3.6 mg/depot) to male rats once every 28 days for 2-24 wk to determine the extent to which pituitary-testis function could be suppressed and whether suppression was maintained throughout the period of treatment. Administration of Zoladex resulted in sustained decreases in weight of the testis, epididymis, seminal vesicles and prostate gland. The decreases were apparent within 2 wk of initiating treatment. Patchy degeneration of the seminiferous tubules and atrophy of the Leydig cells were observed, but did not progress beyond the degree observed after 1 month of treatment. Serum and testis testosterone were markedly depressed after 2 wk of treatment, as was testis [125I]hCG binding. Serum gonadotropins were also reduced by treatment. Serum androgen binding protein (ABP) was elevated, testis ABP content remained unchanged, and epididymal ABP content was reduced. The changes are consistent with the hypothesis that this compound affects both the anterior pituitary gland and the testis. These findings indicate that depot delivery systems are a convenient way to administer GnRH analogs for sustained treatment schedules.
女性服用 GnRH 激动剂后，刺激 LH 片段的生物活性降低。
DOI：
10.1210/jcem-58-4-755
发表时间：
1984
期刊：
The Journal of clinical endocrinology and metabolism
影响因子：
--
作者：
Meldrum,DR;Tsao,Z;Monroe,SE;Braunstein,GD;Sladek,J;Lu,JK;Vale,W;Rivier,J;Judd,HL;Chang,RJ
通讯作者：
Chang,RJ
黄体生成素释放激素激动剂降低人体黄体生成素的生物活性并改变其色谱行为。
DOI：
10.1172/jci111200
发表时间：
1984
期刊：
The Journal of clinical investigation
影响因子：
--
作者：
Evans,RM;Doelle,GC;Lindner,J;Bradley,V;Rabin,D
通讯作者：
Rabin,D
影响因子：
4.8
作者：
MORRIS, ID;PHILLIPS, DM;BARDIN, CW
通讯作者：
BARDIN, CW