Gispen W H, Buitelaar J, Wiegant V M, Terenius L, De Wied D
Eur J Pharmacol. 1976 Oct;39(2):393-7. doi: 10.1016/0014-2999(76)90150-3.
The present study confirms that N-terminal fragments of ACTH have an affinity for rat brain opiate receptors in vitro. Such peptides, devoid of corticotrophic activity, were found to inhibit morphine-induced analgesia if they also possessed affinity for opiate receptors in vitro. The structure-activity relationship for these two parameters is comparable to that observed for the same peptides on the induction of excessive grooming.
本研究证实,促肾上腺皮质激素(ACTH)的N端片段在体外对大鼠脑阿片受体具有亲和力。如果这些缺乏促肾上腺皮质激素活性的肽在体外也对阿片受体具有亲和力,就会发现它们能抑制吗啡诱导的镇痛作用。这两个参数的构效关系与观察到的相同肽诱导过度梳理行为时的构效关系相当。