Schlicker E, Göthert M
Institut für Pharmakologie und Toxikologie, Rheinische Friedrich-Wilhelms-Universität Bonn, Germany.
Brain Res Bull. 1998 Sep 15;47(2):129-32. doi: 10.1016/s0361-9230(98)00068-9.
The noradrenergic neurones of the autonomic nervous system (postganglionic sympathetic neurones) and of the central nervous system are endowed with presynaptic receptors by which noradrenaline release is inhibited by noradrenaline itself (via the alpha2-autoreceptor) and by other transmitters and mediators (via heteroreceptors). Frequently, but not consistently, inhibitory interactions exist between auto- and heteroreceptors. This holds true for the following heteroreceptors: adenosine A1, cannabinoid CB1, dopamine D2/D3, histamine H3, 5-hydroxytryptamine (serotonin) 5-HT(1B), imidazoline, muscarine M2, delta opioid, kappa opioid, mu opioid, orphan opioid (ORL1), prostaglandin EP3, and somatostatin SRIF1. Such interactions (which have also been obtained in human tissue) may, if not considered, prevent the identification of a putative heteroreceptor or the quantitative estimation of the effect mediated by this receptor, and they may explain drug interactions in humans in vivo; many ligands at the alpha2-autoreceptor and at the heteroreceptors may be simultaneously used for therapeutic reasons (e.g., carbachol, clonidine, dopamine, sumatriptan, mianserin, and misoprostol) or abused (e.g., heroin, LSD, and delta9-tetrahydrocannabinol in hashish or marijuana).
自主神经系统（节后交感神经元）和中枢神经系统中的去甲肾上腺素能神经元具有突触前受体，通过这些受体，去甲肾上腺素自身（通过α2-自受体）以及其他递质和介质（通过异受体）可抑制去甲肾上腺素的释放。通常（但并非始终如此），自受体和异受体之间存在抑制性相互作用。以下异受体也是如此：腺苷A1、大麻素CB1、多巴胺D2/D3、组胺H3、5-羟色胺（血清素）5-HT(1B)、咪唑啉、毒蕈碱M2、δ阿片样物质、κ阿片样物质、μ阿片样物质、孤儿阿片样物质（ORL1）、前列腺素EP3和生长抑素SRIF1。如果不考虑这些相互作用，可能会妨碍对假定异受体的识别或对该受体介导效应的定量评估，并且它们可能解释体内人类的药物相互作用；出于治疗原因（例如，卡巴胆碱、可乐定、多巴胺、舒马曲坦、米安色林和米索前列醇）或滥用（例如，海洛因、麦角酸二乙胺以及大麻或大麻中的δ9-四氢大麻酚），α2-自受体和异受体的许多配体可能会同时被使用。
