摘要
Since the discovery of opioid receptors and their endogenous ligands named opioid peptides, it has been established that opiates exert their effects by mimicking effects of three endogenous opioid peptide families (the enkephalins, the endorphins, and the dynorphins). Over last three decades, great advance has been made in understanding the basic physiology of endogenous opioid peptide (EOP) systems and their biogenesis, anatomy, and functions. EOPs and their receptors are expressed in the CNS, the periphery, the gut, and the immune system. The EOPs act as transmitters or modulate synaptic actions of primary transmitters. There are numerous data implicating EOPs in the central and peripheral antinociception, motor activity, feeding, sexual behavior, regulation of body temperature respiration, as well as cardiovascular and gastrointestinal functions. They are known to be released from endocrine organs and are involved in regulation of release of various hormones and modulation of immune functions. EOPs are involved in reward, learning and memory, and emotional states. EOP systems play an important role in modulation and adaptation of the organism to challenges. While relatively quiescent in the resting state, EOPs are released during intense stimulation and modify disturbed homeostasis. EOPs appear to be involved in brain diseases such as pain, addiction, depression, and anxiety disorders. Progress made during the last years in pharmacology, genomics, and complex genetics opens avenues for investigating a role of the EOPs and their receptors in various brain diseases and new pathways for investigating novel opioid therapeutics.
摘要译文
自从发现阿片受体及其内源性配体命名为阿片肽，它已经建立了阿片类药物通过模拟3个内源阿片肽家族（脑啡肽，内啡肽和强啡肽）的作用发挥它们的作用。在过去的三十年中，在理解内源性阿片肽（EOP）系统的基本生理学及其生物发生，解剖学和功能方面取得了很大进展。EOP及其受体在CNS，外周，肠道和免疫系统中表达。 EOP充当发射器或调制主发射器的突触动作。有许多数据暗示EOP在中枢和外周的抗伤害感受，运动活动，摄食，性行为，体温呼吸的调节，以及心血管和胃肠功能。已知它们从内分泌器官释放并参与调节各种激素的释放和免疫功能的调节。 EOP参与奖励，学习和记忆，和情绪状态。 EOP系统在调节和适应生物体对挑战中起着重要作用。虽然在静止状态下相对静止，在强烈刺激期间释放EOP并改变受干扰的体内平衡。 EOP似乎与脑部疾病有关，如疼痛，成瘾，抑郁和焦虑症。最近几年在药理学，基因组学方面取得的进展，复杂的遗传学为研究EOP及其受体在各种脑疾病中的作用以及研究新型阿片类药物疗法的新途径开辟了道路。
Ryszard Przewlocki[1]. Opioid Peptides. Neuroscience in the 21st Century[M].DE: Springer, 2016: 1783-1810