促黄体生成素释放激素拮抗剂在体外对促黄体生成素释放激素诱导的环磷酸腺苷积累以及促黄体生成素和促卵泡激素释放的平行抑制作用。
Parellel inhibition of LH-RH-induced cyclic AMP accumulation and LH and FSH release by LH-RH antagonists in vitro.
作者信息
Beaulieu M, Labrie F, Coy D H, Coy E J, Schally A V
出版信息
J Cyclic Nucleotide Res. 1975;1(6):243-50.
The relative potencies of seven antagonists of LH-RH to inhibit LH-RH-induced cyclic AMP accumulation and LH and FSH release were measured using rat hemipituitaries in vitro. At appropriate concentrations, [Des-His2, D-Ala6] LH-RH, [Des-His2, D-Ala6, des-Gly-NH210] LH-RH ethylamide, [Des-His2, D-Leu6] LH-RH, [D-Phe2] LH-RH, [Des-His2, Des-Gly-NH210] LH-RH propylamide, [D-Phe2, D-Leu6] LH-RH and [D-Phe2, D-Phe6] LH-RH led to parallel inhibition of cyclic AMP accumulation and LH and FSH release. [D-Phe2, D-Leu6] LH-RH and [D-Phe2, D-Phe6] LH-RH can inhibit 50% of LH-RH action at molar ratios of 100 and 30, respectively. These findings of parallel changes of cyclic AMP levels and LH and FSH release add strong support to the already obtained evidence for a mediator role of the adenylate cyclase system in the action of LH-RH in the anterior pituitary gland.
利用大鼠半垂体体外培养法，测定了七种促黄体生成素释放激素（LH-RH）拮抗剂抑制LH-RH诱导的环磷酸腺苷（cAMP）积累以及促黄体生成素（LH）和促卵泡生成素（FSH）释放的相对效价。在适宜浓度下，[去组氨酸2，D-丙氨酸6]LH-RH、[去组氨酸2，D-丙氨酸6，去甘氨酰胺10]LH-RH乙酰胺、[去组氨酸2，D-亮氨酸6]LH-RH、[D-苯丙氨酸2]LH-RH、[去组氨酸2，去甘氨酰胺10]LH-RH丙酰胺、[D-苯丙氨酸2，D-亮氨酸6]LH-RH和[D-苯丙氨酸2，D-苯丙氨酸6]LH-RH可导致对cAMP积累以及LH和FSH释放的平行抑制。[D-苯丙氨酸2，D-亮氨酸6]LH-RH和[D-苯丙氨酸2，D-苯丙氨酸6]LH-RH分别在摩尔比为100和30时可抑制50%的LH-RH作用。cAMP水平以及LH和FSH释放的平行变化这一发现，为已获得的关于腺苷酸环化酶系统在LH-RH于垂体前叶作用中起介质作用的证据提供了有力支持。
Zotero 插件