Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China.
School of basic medicine and clinical pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Biomed Pharmacother. 2016 Oct;83:439-449. doi: 10.1016/j.biopha.2016.07.002. Epub 2016 Jul 15.
Human trace amines (TAs) are endogenous compounds, previously almost ignored in human pathology for many reasons (difficulty of their measurement in biological fluids, unknown receptors for elusive amines), are now considered to play a significant role in synaptic transmission within the central nervous system (CNS) acting as neuromodulators. 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. Human trace amine receptors (including TAAR1 TAAR2 TAAR5 TAAR6 TAAR8 TAAR9) are expressed in the brain and play significant physiological and neuropathological roles by activation of trace amines. We herein discuss the recent findings that provide insights into the functional roles of human trace amines (including P-Octopamine, β phenylethylamine, Tryptamine, Tyramine, Synephrine, 3-Iodothyronamine, 3-Methoxytyramine, N-Methyltyramine, N-Methylphenethylamine) in brain. Furthermore, we discuss the known functions of human trace amine receptors in brain.
人体微量胺(TAs)是内源性化合物,由于多种原因(在生物体液中测量困难,对难以捉摸的胺类的未知受体),在过去很长一段时间内几乎被忽略,但现在被认为在中枢神经系统(CNS)内的突触传递中发挥重要作用,作为神经调质。最近发现了一类新型的 G 蛋白偶联受体(GPCRs),其中包括对 TAs 具有高度特异性的个体成员,这表明 TAs 可能作为脊椎动物神经递质或神经调质发挥作用,尽管迄今为止,这些 GPCRs 中的大多数尚未被证明可被 TAs 激活。人体微量胺受体(包括 TAAR1、TAAR2、TAAR5、TAAR6、TAAR8、TAAR9)在大脑中表达,并通过激活微量胺发挥重要的生理和神经病理学作用。我们在此讨论了最近的发现,这些发现深入了解了人体微量胺(包括 P-章鱼胺、β-苯乙胺、色胺、酪胺、辛弗林、3-碘甲状腺素、3-甲氧基酪胺、N-甲基酪胺、N-甲基苯乙胺)在大脑中的功能作用。此外,我们还讨论了已知的人体微量胺受体在大脑中的功能。