Gold M S, Byck R, Sweeney D R, Kleber H D
Biomedicine. 1979 Feb;30(1):1-4.
Endorphins and exogenous opiates inhibit the activity of the noradrenergic nucleus locus coeruleus (LC). This discovery of endorphin transmitters and their interaction with the LC has supported our studies which have suggested that the majority of the signs and symptoms of opiate withdrawal are mimicked by electrical or chemical activation of the LC. We hypothesize that this endorphin-LC connection is critical to opiate action and the withdrawal syndrome. This hypothesis suggests that chronic opiate administration inhibits LC activity and that opiate abstinence after addiction results in a release from inhibition with resultant LC hyperactivity. This hypothesis is supported by recent data suggesting that clonidine as a drug which inhibits the LC and LC-mediated noradrenergic activation, is an efficacious non-opiate treatment for opiate withdrawal. This hypothesis can be tested in man by evaluating drugs which inhibit the LC and LC-mediated behaviors for anti-withdrawal efficacy.
内啡肽和外源性阿片类物质会抑制去甲肾上腺素能蓝斑核（LC）的活性。内啡肽递质的这一发现及其与蓝斑核的相互作用，为我们的研究提供了支持，我们的研究表明，阿片类药物戒断的大多数体征和症状可通过电刺激或化学刺激蓝斑核来模拟。我们推测，这种内啡肽-蓝斑核联系对阿片类药物作用和戒断综合征至关重要。这一假说表明，长期服用阿片类药物会抑制蓝斑核活性，成瘾后停用阿片类药物会导致抑制解除，从而使蓝斑核活动亢进。最近的数据支持了这一假说，这些数据表明，可乐定作为一种抑制蓝斑核和蓝斑核介导的去甲肾上腺素能激活的药物，是一种有效的非阿片类药物戒断治疗方法。这一假说可通过评估抑制蓝斑核和蓝斑核介导行为的药物的抗戒断疗效在人体中进行检验。
