Bhargava H N, Yousif D J, Matwyshyn G A
Gen Pharmacol. 1983;14(6):565-70. doi: 10.1016/0306-3623(83)90150-7.
The interactions of thyrotropin releasing hormone, its metabolites and synthetic analogues with acute and chronic effects of endogenous and exogenous opiates have been described. The endogenous and exogenous opiates are represented by beta-endorphin and morphine, respectively. The pharmacological effects of opiates include analgesia, temperature effects, respiratory depression, catalepsy, locomotor activity, opiate receptor binding, tolerance, and physical dependence. Thyrotropin releasing hormone and related compounds appear to (a) antagonize hypothermia, respiratory depression, locomotor depression and catalepsy but not the analgesia induced by opiates, (b) inhibit the development of tolerance to the analgesic effect but not to the hypothermic effect of opiates, (c) inhibit the development of physical dependence on opiates as evidenced by the inhibition of development of certain withdrawal symptoms, and (d) suppress the abstinence syndrome in opiate dependent rodents. Thyrotropin releasing hormone does not interact with the opiate receptors in the brain. Potential therapeutic applications of thyrotropin releasing hormone and its synthetic analogues in counteracting some of the undesirable effects of opiates are discussed.
促甲状腺激素释放激素、其代谢产物及合成类似物与内源性和外源性阿片类药物的急性和慢性效应之间的相互作用已被描述。内源性和外源性阿片类药物分别以β-内啡肽和吗啡为代表。阿片类药物的药理作用包括镇痛、体温效应、呼吸抑制、僵住症、运动活性、阿片受体结合、耐受性和身体依赖性。促甲状腺激素释放激素及相关化合物似乎（a）拮抗体温过低、呼吸抑制、运动抑制和僵住症，但不拮抗阿片类药物诱导的镇痛作用，（b）抑制对镇痛作用的耐受性发展，但不抑制对阿片类药物体温过低效应的耐受性发展，（c）抑制对阿片类药物身体依赖性的发展，如通过抑制某些戒断症状的发展所证明，以及（d）抑制阿片类药物依赖的啮齿动物的戒断综合征。促甲状腺激素释放激素不与大脑中的阿片受体相互作用。讨论了促甲状腺激素释放激素及其合成类似物在对抗阿片类药物一些不良效应方面的潜在治疗应用。
