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TAAR 激动剂。

TAAR Agonists.

机构信息

Collaborative Innovation Center for Brain Science, Department of Anatomy and Physiology, Shanghai Jiao Tong University School of Medicine, Shanghai, 200025, China.

Department of Otolaryngology Head and Neck Surgery, Jiangsu Provincial Key Medical Discipline (Laboratory), Affiliated Drum Tower Hospital of Nanjing University Medical School, Nanjing, 210008, China.

出版信息

Cell Mol Neurobiol. 2020 Mar;40(2):257-272. doi: 10.1007/s10571-019-00774-5. Epub 2019 Dec 17.

DOI:10.1007/s10571-019-00774-5
PMID:31848873
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11449014/
Abstract

Trace amine-associated receptors (TAARs) are a family of G protein-coupled receptors (GPCRs) that are evolutionarily conserved in vertebrates. The first discovered TAAR1 is mainly expressed in the brain, and is able to detect low abundant trace amines. TAAR1 is also activated by several synthetic compounds and psychostimulant drugs like amphetamine. Activation of TAAR1 by specific agonists can regulate the classical monoaminergic systems in the brain. Further studies have revealed that other TAAR family members are highly expressed in the olfactory system which are termed olfactory TAARs. In vertebrates, olfactory TAARs can specifically recognize volatile or water-soluble amines. Some of these TAAR agonists are produced by decarboxylation of amino acids. In addition, some TAAR agonists are ethological odors that mediate animal innate behaviors. In this study, we provide a comprehensive review of TAAR agonists, including their structures, biosynthesis pathways, and functions.

摘要

痕量胺相关受体(TAARs)是一组在脊椎动物中进化保守的 G 蛋白偶联受体(GPCRs)。第一个被发现的 TAAR1 主要在大脑中表达,能够检测低丰度的痕量胺。TAAR1 也被几种合成化合物和安非他命等精神兴奋剂激活。特定激动剂激活 TAAR1 可以调节大脑中的经典单胺能系统。进一步的研究表明,其他 TAAR 家族成员在嗅觉系统中高度表达,被称为嗅觉 TAARs。在脊椎动物中,嗅觉 TAARs 可以特异性识别挥发性或水溶性胺。其中一些 TAAR 激动剂是由氨基酸脱羧产生的。此外,一些 TAAR 激动剂是行为气味,介导动物先天行为。在这项研究中,我们提供了 TAAR 激动剂的全面综述,包括它们的结构、生物合成途径和功能。

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引用本文的文献

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2
Structural bioinformatic study of six human olfactory receptors and their AlphaFold3 predicted water-soluble QTY variants and OR1A2 with an odorant octanoate and TAAR9 with spermidine.六种人类嗅觉受体及其AlphaFold3预测的水溶性QTY变体、与辛酸结合的OR1A2以及与亚精胺结合的TAAR9的结构生物信息学研究。
QRB Discov. 2024 Dec 9;6:e2. doi: 10.1017/qrd.2024.18. eCollection 2025.
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Regulation by Trace Amine-Associated Receptor 1 (TAAR1) of Dopaminergic-GABAergic Interaction in the Striatum: Effects of the Enhancer Drug (-)BPAP.纹状体中多巴胺能-γ-氨基丁酸能相互作用受痕量胺相关受体1(TAAR1)的调节:增强剂药物(-)BPAP的作用
Neurochem Res. 2025 Feb 4;50(2):94. doi: 10.1007/s11064-025-04337-7.
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Molecular Mechanisms of Methamphetamine-Induced Addiction via TAAR1 Activation.通过 TAAR1 激活导致甲基苯丙胺成瘾的分子机制。
J Med Chem. 2024 Oct 24;67(20):18593-18605. doi: 10.1021/acs.jmedchem.4c01961. Epub 2024 Oct 2.
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本文引用的文献

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Amphetamines signal through intracellular TAAR1 receptors coupled to Gα and Gα in discrete subcellular domains.安非他命通过与Gα和Gα偶联的细胞内TAAR1受体在离散的亚细胞结构域中发出信号。
Mol Psychiatry. 2021 Apr;26(4):1208-1223. doi: 10.1038/s41380-019-0469-2. Epub 2019 Aug 9.
2
Effects of an Extract of Salmon Milt on Symptoms and Serum TNF and Substance P in Patients With Fibromyalgia Syndrome.三文鱼精子提取物对纤维肌痛综合征患者症状及血清 TNF 和 P 物质的影响。
Clin Ther. 2019 Aug;41(8):1564-1574.e2. doi: 10.1016/j.clinthera.2019.05.019. Epub 2019 Jul 11.
3
Spermine in semen of male sea lamprey acts as a sex pheromone.精胺在雄性海七鳃鳗精液中起性信息素的作用。
PLoS Biol. 2019 Jul 9;17(7):e3000332. doi: 10.1371/journal.pbio.3000332. eCollection 2019 Jul.
4
Pharmacological profiles of compounds in preworkout supplements ("boosters").运动前补充剂(“助推剂”)中化合物的药理学特性。
Eur J Pharmacol. 2019 Sep 15;859:172515. doi: 10.1016/j.ejphar.2019.172515. Epub 2019 Jun 29.
5
The best smellers make the best choosers: mate choice is affected by female chemosensory receptor gene diversity in a mammal.嗅觉最好的动物做出的选择最好:在哺乳动物中,雌性化学感受器受体基因多样性会影响配偶选择。
Proc Biol Sci. 2018 Dec 19;285(1893):20182426. doi: 10.1098/rspb.2018.2426.
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White shark genome reveals ancient elasmobranch adaptations associated with wound healing and the maintenance of genome stability.白鲨基因组揭示了与创伤愈合和基因组稳定性维持相关的古老软骨鱼适应性。
Proc Natl Acad Sci U S A. 2019 Mar 5;116(10):4446-4455. doi: 10.1073/pnas.1819778116. Epub 2019 Feb 19.
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Trace amine-associated receptor 1 (TAAR1) promotes anti-diabetic signaling in insulin-secreting cells.痕量胺相关受体 1(TAAR1)促进胰岛素分泌细胞中的抗糖尿病信号传导。
J Biol Chem. 2019 Mar 22;294(12):4401-4411. doi: 10.1074/jbc.RA118.005464. Epub 2019 Jan 22.
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Endocr Rev. 2019 Apr 1;40(2):602-630. doi: 10.1210/er.2018-00182.