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

ABSTRACT: 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.

SUBMITTER: Maguire JJ

PROVIDER: S-EPMC2830119 | biostudies-literature | 2009 Mar

REPOSITORIES: biostudies-literature

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

Maguire Janet J JJ Parker William A E WA Foord Steven M SM Bonner Tom I TI Neubig Richard R RR Davenport Anthony P AP

Pharmacological reviews 20090301 1

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 r ...[more]

PMID: 19325074

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Project description:The calcium-sensing receptor (CaSR) is a class C G protein-coupled receptor that responds to multiple endogenous agonists and allosteric modulators, including divalent and trivalent cations, L-amino acids, γ-glutamyl peptides, polyamines, polycationic peptides, and protons. The CaSR plays a critical role in extracellular calcium (Ca2+ o) homeostasis, as demonstrated by the many naturally occurring mutations in the CaSR or its signaling partners that cause Ca2+ o homeostasis disorders. However, CaSR tissue expression in mammals is broad and includes tissues unrelated to Ca2+ o homeostasis, in which it, for example, regulates the secretion of digestive hormones, airway constriction, cardiovascular effects, cellular differentiation, and proliferation. Thus, although the CaSR is targeted clinically by the positive allosteric modulators (PAMs) cinacalcet, evocalcet, and etelcalcetide in hyperparathyroidism, it is also a putative therapeutic target in diabetes, asthma, cardiovascular disease, and cancer. The CaSR is somewhat unique in possessing multiple ligand binding sites, including at least five putative sites for the "orthosteric" agonist Ca2+ o, an allosteric site for endogenous L-amino acids, two further allosteric sites for small molecules and the peptide PAM, etelcalcetide, and additional sites for other cations and anions. The CaSR is promiscuous in its G protein-coupling preferences, and signals via Gq/11, Gi/o, potentially G12/13, and even Gs in some cell types. Not surprisingly, the CaSR is subject to biased agonism, in which distinct ligands preferentially stimulate a subset of the CaSR's possible signaling responses, to the exclusion of others. The CaSR thus serves as a model receptor to study natural bias and allostery. SIGNIFICANCE STATEMENT: The calcium-sensing receptor (CaSR) is a complex G protein-coupled receptor that possesses multiple orthosteric and allosteric binding sites, is subject to biased signaling via several different G proteins, and has numerous (patho)physiological roles. Understanding the complexities of CaSR structure, function, and biology will aid future drug discovery efforts seeking to target this receptor for a diversity of diseases. This review summarizes what is known to date regarding key structural, pharmacological, and physiological features of the CaSR.

Dataset Information

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

Publications

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

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