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International Union of Pharmacology. LXXII. Recommendations for trace amine receptor nomenclature.

机译:国际药理学联合会。 LXXII。微量胺受体命名的建议。

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Trace amines such as p-tyramine and beta-phenylethylamine are found endogenously as well as in the diet. Concomitant ingestion of these foodstuffs with monoamine oxidase inhibitors may result in the hypertensive crisis known as the "beer, wine, and cheese effect" attributed to their sympathomimetic action. Trace amines have been shown to act on one of a novel group of mammalian seven transmembrane spanning G protein-coupled receptors belonging to the rhodopsin superfamily, cloned in 2001. This receptor encoded by the human TAAR1 gene is also present in rat and mouse genomes (Taar1) and has been shown to be activated by endogenous trace amine ligands, including p-tyramine and beta-phenylethylamine. A number of drugs, most notably amphetamine and its derivatives, act as agonists at this receptor. This review proposes an official nomenclature designating TAAR1 as the trace amine 1 receptor following the convention of naming receptors after the endogenous agonist, abbreviated to TA(1) where necessary. It goes on to discuss briefly the significance of the receptor, agents acting upon it, its distribution, and currently hypothesized physiological and pathophysiological roles. In humans, a further five genes are thought to encode functional receptors (TAAR2, TAAR5, TAAR6, TAAR8, and TAAR9). TAAR3 seems to be a pseudogene in some individuals but not others. TAAR4 is a pseudogene in humans, but occurs with TAAR3 as a functional gene in rodents. Nine further genes are present in rats and mice. The endogenous ligands are not firmly established but some may respond to odorants consistent with their expression in olfactory epithelium.
机译:内源性以及饮食中都发现了痕量胺,例如对酪胺和β-苯乙胺。这些食物与单胺氧化酶抑制剂同时摄入可能导致高血压危机,这是由于其拟交感神经作用而引起的“啤酒,葡萄酒和奶酪效应”。微量胺已被证明可作用于2001年克隆的,属于视紫红质超家族的一组新的哺乳动物跨膜蛋白跨接G蛋白的七个新受体之一。该人TAAR1基因编码的受体也存在于大鼠和小鼠基因组中( Taar1),并已被内源性痕量胺配体激活,包括对-酪胺和β-苯乙胺。许多药物,尤其是苯丙胺及其衍生物,在该受体上起激动剂的作用。这篇综述提出了一个官方命名法,将TAAR1指定为内源性激动剂后命名受体的惯例,作为痕量胺1受体,必要时缩写为TA(1)。继续简要讨论了受体的重要性,作用于受体的药剂,其分布以及目前假设的生理和病理生理作用。在人类中,另外五个基因被认为编码功能性受体(TAAR2,TAAR5,TAAR6,TAAR8和TAAR9)。 TAAR3在某些个体中似乎是假基因,但在其他个体中不是。 TAAR4是人类的假基因,但与TAAR3作为啮齿动物的功能基因一起出现。大鼠和小鼠中还存在9个其他基因。内源性配体尚未牢固建立,但有些可能会对与嗅觉上皮中表达一致的气味产生反应。

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