Lindemann Lothar, Hoener Marius C
F. Hoffmann-La Roche, Pharmaceuticals Division, Discovery Neuroscience, CH-4070-Basel, Switzerland.
Trends Pharmacol Sci. 2005 May;26(5):274-81. doi: 10.1016/j.tips.2005.03.007.
Trace amines (TAs) are endogenous compounds that are related to biogenic amine neurotransmitters and are present in the mammalian nervous system in trace amounts. Although their pronounced pharmacological effects and tight link to major human disorders such as depression and schizophrenia have been studied for decades, the understanding of their molecular mode of action remained incomplete because of the apparent absence of specialized receptors. However, the recent discovery of a novel family of G-protein-coupled receptors (GPCRs) that includes individual members that are highly specific for TAs indicates a potential role for TAs as vertebrate neurotransmitters or neuromodulators, although the majority of these GPCRs so far have not been demonstrated to be activated by TAs. The unique pharmacology and expression pattern of these receptors make them prime candidates for targets in drug development in the context of several neurological diseases. Current research focuses on dissecting their molecular pharmacology and on the identification of endogenous ligands for the apparently TA-insensitive members of this receptor family.
痕量胺（TAs）是与生物胺神经递质相关的内源性化合物，以痕量存在于哺乳动物神经系统中。尽管它们显著的药理作用以及与抑郁症和精神分裂症等主要人类疾病的紧密联系已被研究了数十年，但由于明显缺乏专门的受体，对其分子作用模式的理解仍不完整。然而，最近发现了一个新的G蛋白偶联受体（GPCRs）家族，其中包括对TAs具有高度特异性的个体成员，这表明TAs作为脊椎动物神经递质或神经调节剂具有潜在作用，尽管到目前为止，这些GPCRs中的大多数尚未被证明能被TAs激活。这些受体独特的药理学和表达模式使其成为几种神经疾病药物开发中靶点的主要候选者。目前的研究重点是剖析它们的分子药理学，并确定该受体家族中对TAs不敏感的成员的内源性配体。
