INVOLVEMENT OF THE MU-OPIATE RECEPTOR IN PERIPHERAL ANALGESIA
INVOLVEMENT OF THE MU-OPIATE RECEPTOR IN PERIPHERAL ANALGESIA
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DOI：
10.1016/0306-4522(89)90279-0
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发表时间：
1989-01-01
期刊：
影响因子：
3.3
通讯作者：
TAIWO, YO
中科院分区：
文献类型：
--
作者：
LEVINE, JD;TAIWO, YO
皮内注射μ（吗啡、Tyr-D-Ala-Gly-NMe-Phe-Gly-ol和morphiceptin）、κ（反式-3，4-二氯-N-甲基-N-[2-（1-吡咯烷基）环己基]苯乙酰胺）和δ [D-Pen 2.5]-脑啡肽和[D-Ser 2]-[Leu]脑啡肽-Thr）选择性阿片样物质激动剂本身并不显著影响大鼠后爪的机械伤害感受阈值。皮内注射μ，但不是δ或κ阿片样物质激动剂，然而，产生剂量依赖性抑制前列腺素E2诱导的痛觉过敏。吗啡的镇痛作用可被纳洛酮剂量依赖性地拮抗，并可被百日咳毒素阻断。然而，吗啡并没有改变8-溴环磷酸腺苷引起的痛觉过敏。我们的结论是阿片类药物对初级传入神经末梢的镇痛作用是通过一个具有μ阿片受体特征的结合位点，并且这种作用是通过抑制环磷酸腺苷第二信使系统介导的。
The intradermal injection of mu (morphine, Tyr-D-Ala-Gly-NMe-Phe-Gly-ol and morphiceptin), kappa (trans-3,4-dichloro-N-methyl-N[2-(1--pyroolidinyl)cyclohexyl]benzeneactemide) and delta [D-Pen2.5]-enkephalin and [D-Ser2]-[Leu]enkephalin-Thr) selective opioid-agonists, by themselves, did not significantly affect the mechanical nociceptive threshold in the hindpaw of the rat. Intradermal injection of mu, but not delta or kappa opioid-agonists, however, produced dose-dependent inhibition of prostaglandin E2-induced hyperalgesia. The analgesic effect of the mu-agonist morphine was dose-dependently antagonized by naloxone and prevented by co-injection of pertussis toxin. Morphine did not, however, alter the hyperalgesia induced by 8-bromo cyclic adenosine monophosphate. We conclude that the analgesic action of opioids on the peripheral terminals of primary afferents is via a binding site with characteristics of the mu-opioid receptor and that this action is mediated by inhibition of the cyclic adenosine monophosphate second messenger system.