Pfeiffer D G, Pfeiffer A, Shimohigashi Y, Merriam G R, Loriaux D L
Peptides. 1983 Sep-Oct;4(5):647-9. doi: 10.1016/0196-9781(83)90012-8.
Opiate alkaloids and opioid peptides have been shown to suppress plasma LH and FSH levels via a naloxone sensitive mechanism in several species including man. Three subtypes of opiate receptors have been characterized: mu, delta and kappa. The present study was designed to investigate their role in gonadotropin release. Three highly selective opioid ligands, DAGO, MRZ and DTE12 (a dimeric tetrapeptide enkephalin), were injected intraventricularly into chronically ovariectomized rats. Injection of the mu-agonist at doses of 1 and 10 nmol produced a significant suppression of LH secretion, while the delta- and kappa-agonists had no significant effect. Thus, the mu-receptor seems to be the primary opiate receptor involved in the regulation of LH secretion. None of the opiate agonists employed had an effect on FSH secretion.
阿片生物碱和阿片肽已被证明，在包括人类在内的多个物种中，可通过一种纳洛酮敏感机制抑制血浆促黄体生成素（LH）和促卵泡生成素（FSH）水平。阿片受体有三种亚型：μ、δ和κ。本研究旨在探讨它们在促性腺激素释放中的作用。将三种高度选择性的阿片类配体，即DAGO、MRZ和DTE12（一种二聚体四肽脑啡肽），脑室内注射到长期卵巢切除的大鼠体内。以1和10纳摩尔的剂量注射μ激动剂可显著抑制LH分泌，而δ和κ激动剂则无显著作用。因此，μ受体似乎是参与LH分泌调节的主要阿片受体。所使用的阿片类激动剂均对FSH分泌无影响。
