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强啡肽与外周阿片受体的相互作用。

Dermorphin interaction with peripheral opioid receptors.

作者信息

Giagnoni G, Parolaro D, Casiraghi L, Crema G, Sala M, Andreis C, Gori E

出版信息

Neuropeptides. 1984 Dec;5(1-3):157-60. doi: 10.1016/0143-4179(84)90051-9.

Abstract

The interaction of dermorphin with different peripheral opioid receptor subtypes was investigated in vitro, using the guinea pig ileum as representative tissue for mu, the mouse vas deferens for delta, the rabbit vas deferens for kappa and the rat vas deferens for epsilon. The effect of dermorphin on each tissue preparation was compared with that of selective mu, delta, kappa epsilon agonists respectively morphine, met-enkephalinamide, ethylketocyclazocine and camel beta-endorphin. Antagonism with naloxone was also tested and calculated as Ke. It is concluded that dermorphin mainly interacts with the mu receptors, although it also binds to epsilon receptors; the interaction with delta receptors is questionable, and the kappa receptors are unaffected.

摘要

利用豚鼠回肠作为μ受体的代表性组织、小鼠输精管作为δ受体的代表性组织、兔输精管作为κ受体的代表性组织、大鼠输精管作为ε受体的代表性组织,在体外研究了皮啡肽与不同外周阿片受体亚型的相互作用。将皮啡肽对每种组织制剂的作用分别与选择性μ、δ、κ、ε激动剂吗啡、甲硫氨酸脑啡肽酰胺、乙基酮环唑辛和骆驼β-内啡肽的作用进行比较。还测试了与纳洛酮的拮抗作用,并计算为Ke。得出的结论是,皮啡肽主要与μ受体相互作用,尽管它也与ε受体结合;与δ受体的相互作用存在疑问,κ受体未受影响。

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