Corbin A, Beattie C W
Endocrinology. 1976 Jan;98(1):247-50. doi: 10.1210/endo-98-1-247.
Stalk-medium eminence (SME) and plasma LHRH activities of chronically hypophysectomized immature female rats were evaluated by bioassay following a single subcutaneous injection of varying doses of either LHRH or the LHRH antagonist, [D-Phe2, D-Ala6]-LHRH (Wy-18,185). Administration of LHRH to hypophysectomized rats produced parallel dose-related increases in SME and plasma LHRH activities. Wy-18,185 produced a similar, but attenuated dose-related increase in SME-LHRH activity, while a dose-related decrease in plasma LHRH activity was observed. Collectively, the data suggest that (1) exogenous LHRH may be sequestered by the hypothalamus leading to significant increases in hypothalamic LHRH content, and (2) peptide antagonists of LHRH inhibit the release of endogenous LHRH at the hypothalamic level.
对慢性垂体切除的未成熟雌性大鼠,在单次皮下注射不同剂量的促黄体生成素释放激素(LHRH)或LHRH拮抗剂[D-苯丙氨酸2,D-丙氨酸6]-LHRH(Wy-18,185)后,通过生物测定法评估茎-中间隆起(SME)和血浆LHRH活性。给垂体切除的大鼠注射LHRH后,SME和血浆LHRH活性呈平行的剂量相关增加。Wy-18,185使SME-LHRH活性产生类似但减弱的剂量相关增加,同时观察到血浆LHRH活性呈剂量相关下降。总体而言,数据表明:(1)外源性LHRH可能被下丘脑隔离,导致下丘脑LHRH含量显著增加;(2)LHRH肽拮抗剂在下丘脑水平抑制内源性LHRH的释放。