Lam Vincent M, Espinoza Stefano, Gerasimov Andrey S, Gainetdinov Raul R, Salahpour Ali
Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada.
Department of Neuroscience and Brain Technologies, Istituto Italiano di Tecnologia, Genova, Italy.
Eur J Pharmacol. 2015 Sep 15;763(Pt B):136-42. doi: 10.1016/j.ejphar.2015.06.026. Epub 2015 Jun 17.
Trace-amines (TAs) are endogenous amines that are implicated in several physiological processes including modulation of aminergic neurotransmission. These compounds exert their effect by activating a class of G protein-coupled receptors termed Trace-Amine Associated Receptors (TAARs), where TAAR1 is the only human receptor that has been shown to bind endogenous TAs. Most of the studies have focused on studying the role of TAAR1 on modulation of the dopamine transmission. These studies indicate that TAAR1 is a negative regulator of dopamine transmission making TAAR1 a novel target for neuropsychiatric disorders that arises from dopamine dysfunction such as schizophrenia. This review discusses the unique pharmacology of TAAR1 with the major focus on the physiological role of TAAR1 and its modulation of dopamine transmission.
痕量胺(TAs)是内源性胺类,参与多种生理过程,包括调节胺能神经传递。这些化合物通过激活一类称为痕量胺相关受体(TAARs)的G蛋白偶联受体发挥作用,其中TAAR1是唯一已被证明能结合内源性TAs的人类受体。大多数研究集中于研究TAAR1在多巴胺传递调节中的作用。这些研究表明,TAAR1是多巴胺传递的负调节因子,这使得TAAR1成为因多巴胺功能障碍(如精神分裂症)引起的神经精神疾病的新靶点。本综述讨论了TAAR1独特的药理学,主要关注TAAR1的生理作用及其对多巴胺传递的调节。