Schwartz J C, Arrang J M, Garbarg M, Korner M
J Exp Biol. 1986 Sep;124:203-24. doi: 10.1242/jeb.124.1.203.
In brain, histamine (HA) is the transmitter of a neuronal system resembling other monoaminergic systems. It is also present in mast cells from which it may control vascular and inflammatory processes. Its various actions are mediated not only by the two well known H1- and H2-receptor subclasses but also by the recently discovered H3-receptors, with distinct localization and pharmacology. H1-receptors mediate a series of biochemical responses which have several features in common: they require intact cells to be observed and largely depend upon the availability of Ca2+. H1-receptor-mediated responses include glycogenolysis, stimulation of cyclic GMP formation, potentiation of cyclic AMP formation. Recent studies indicate that H1-receptors are linked with phosphatidylinositol breakdown and generation of two intracellular signals which both contribute to the final response (e.g. in the cyclic AMP generation). H2-receptors seem to be directly linked with an adenylate cyclase and their stimulation results in enhanced electrophysiologically recorded responses to excitatory agents. Finally whereas H1- and H2-receptors appear to be postsynaptically located, a novel subclass (H3) of HA receptors was recently revealed with a presynaptic localization. H3-receptors are autoreceptors mediating inhibition of HA release from and biosynthesis in histaminergic nerve terminals in the CNS. The physiological and pharmacological implications of three distinct receptor subclasses for HA will be discussed.
在大脑中，组胺（HA）是一个类似于其他单胺能系统的神经元系统的递质。它也存在于肥大细胞中，可能在其中控制血管和炎症过程。其各种作用不仅由两个众所周知的H1和H2受体亚类介导，还由最近发现的具有独特定位和药理学特性的H3受体介导。H1受体介导一系列具有若干共同特征的生化反应：它们需要完整的细胞才能被观察到，并且在很大程度上取决于Ca2+的可用性。H1受体介导的反应包括糖原分解、刺激环鸟苷酸形成、增强环腺苷酸形成。最近的研究表明，H1受体与磷脂酰肌醇分解以及两种细胞内信号的产生有关，这两种信号都对最终反应有贡献（例如在环腺苷酸产生中）。H2受体似乎直接与腺苷酸环化酶相连，它们的刺激导致对兴奋性药物的电生理记录反应增强。最后，虽然H1和H2受体似乎位于突触后，但最近发现了HA受体的一个新亚类（H3），其位于突触前。H3受体是自身受体，介导中枢神经系统中组胺能神经末梢释放和生物合成的HA的抑制。将讨论HA的三种不同受体亚类的生理和药理学意义。
