（D-苯丙氨酸2，D-亮氨酸6）-促黄体激素释放激素和（D-苯丙氨酸2，D-丙氨酸6）-促黄体激素释放激素的抗促黄体激素/促卵泡激素释放激素及抗排卵活性比较

Comparison of the anti-LH/FSH-RH and anti-ovulatory activities of (D-Phe2, D-Leu6)-LH-RH and (D-Phe2, D-Ala6)-LH-RH.

作者信息

Vilchez-Martinez J A, Coy D H, Coy E J, Arimura A, Schally A V

出版信息

Endocr Res Commun. 1976;3(3-4):231-41. doi: 10.3109/07435807609056903.

Abstract

The anti-LH/FSH-RH and antiovulatory activities of [D-Phe2, D-Leu6]-LH-RH and [D-Phe2, D-Ala6]-LH-RH were compared in rats. Both peptides inhibited the LH and FSH release induced by LH-RH in immature male rats, but, 4 hr after the injection, [D-Phe2, D-Leu6]-LH-RH still suppressed the LH and FSH release whereas the [D-Phe2, D-Ala6]-LH-RH did not. When the peptides were administered in equal doses on the afternoon of the day of proestrus in 4-day cycling rats, [D-Phe2, D-Leu6]-LH-RH more completely inhibited the ovulation occurring on the following morning than [D-Phe2, D-Ala6]-LH-RH. Thus, the incorporation of D-Leucine into position six of the decapeptide chain gives a more potent inhibitor than that resulting from the insertion of D-Alanine.

摘要

在大鼠中比较了[D-苯丙氨酸2，D-亮氨酸6]-促黄体生成素释放激素（LH-RH）和[D-苯丙氨酸2，D-丙氨酸6]-LH-RH的抗促黄体生成素/促卵泡激素释放激素（LH/FSH-RH）及抗排卵活性。两种肽均抑制未成熟雄性大鼠中由LH-RH诱导的促黄体生成素（LH）和促卵泡激素（FSH）释放，但是，注射后4小时，[D-苯丙氨酸2，D-亮氨酸6]-LH-RH仍抑制LH和FSH释放，而[D-苯丙氨酸2，D-丙氨酸6]-LH-RH则无此作用。当在4日周期大鼠的动情前期下午以等剂量给予这些肽时，[D-苯丙氨酸2，D-亮氨酸6]-LH-RH比[D-苯丙氨酸2，D-丙氨酸6]-LH-RH更完全地抑制次日早晨发生的排卵。因此，在十肽链的第6位引入D-亮氨酸比插入D-丙氨酸产生的抑制剂更有效。