Crain S M, Shen K F
Department of Neuroscience, Albert Einstein College of Medicine, Yeshiva University, Bronx, NY 10461.
Trends Pharmacol Sci. 1990 Feb;11(2):77-81. doi: 10.1016/0165-6147(90)90322-y.
Activation of opioid receptors has generally been considered to produce inhibitory effects on neuronal activity. However, recent studies indicate that specific mu-, delta- and kappa-opioid receptor agonists can elicit excitatory, as well as inhibitory, modulation of the action potentials of sensory neurons isolated in culture. Stanley Crain and Ke-Fei Shen review the evidence for mediation of these direct excitatory effects by naloxone-reversible opioid receptors. They propose that this dual modulatory mechanism may help to account for previously unexplained enhancement by opioids of transmitter release, paradoxical hyperalgesic and aversive effects of opioids, and some aspects of opioid tolerance and addiction.
阿片受体的激活通常被认为会对神经元活动产生抑制作用。然而，最近的研究表明，特定的μ-、δ-和κ-阿片受体激动剂可以对培养中分离出的感觉神经元的动作电位产生兴奋性以及抑制性调节。斯坦利·克莱恩和沈克非综述了纳洛酮可逆性阿片受体介导这些直接兴奋作用的证据。他们提出，这种双重调节机制可能有助于解释阿片类药物以前无法解释的递质释放增强、阿片类药物矛盾性痛觉过敏和厌恶效应，以及阿片类药物耐受性和成瘾的某些方面。
