Trace amine-associated receptor

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Template:Short description Script error: No such module "redirect hatnote". Template:Use dmy dates Trace amine-associated receptors (TAARs), sometimes referred to as trace amine receptors (TAs or TARs), are a class of G protein-coupled receptors that were discovered in 2001.[1][2] TAAR1, the first of six functional human TAARs, has gained considerable interest in academic and proprietary pharmaceutical research due to its role as the endogenous receptor for the trace amines phenethylamine, tyramine, and tryptamine – metabolic derivatives of the amino acids phenylalanine, tyrosine and tryptophan, respectively – ephedrine, as well as the synthetic psychostimulants, amphetamine, methamphetamine and methylenedioxymethamphetamine (MDMA, ecstasy).[3][4][5][6][7][8] In 2004, it was shown that mammalian TAAR1 is also a receptor for thyronamines, decarboxylated and deiodinated relatives of thyroid hormones.[5] TAAR2–TAAR9 function as olfactory receptors for volatile amine odorants in vertebrates.[9]

Animal TAAR complement

The following is a list of the TAARs contained in selected animal genomes:[10][11]

Human trace amine-associated receptors

Six human trace amine-associated receptors (hTAARs) – hTAAR1, hTAAR2, hTAAR5, hTAAR6, hTAAR8, and hTAAR9 – have been identified and partially characterized. The table below contains summary information from literature reviews, pharmacology databases, and supplementary primary research articles on the expression profiles, signal transduction mechanisms, ligands, and physiological functions of these receptors.

The pharmacology and molecular biology of human trace amine-associated receptors
TAAR
subtype 		Prior
names 		Signal
transduction 		Expression
profile 		Known or putative function in humans[note 1] Known ligands Sources
hTAAR1 TA1
TAR1 		Gs, Gq,
GIRKs,
β-arrestin 2 		CNS: brain (widespread), spinal cord
Periphery: pancreatic β-cells, stomach, duodenum, intestines, leukocytes, elsewhere[note 2] 		Template:BullCNS: modulation of monoamine/glutamate neurotransmission
Template:BullCNS: regulation of cognitive processes & mood states
Template:BullPeriphery: leukocyte chemotaxis
Template:BullPeriphery: regulation of GI hormone release & blood glucose
Template:BullRegulation of satiety & body weight 		Template:BullTrace amines (e.g., tyramine, PEA, NMPEA)
Template:BullMonoamine neurotransmitters (e.g., dopamine)
Template:BullAmphetamine and some structural analogs 		[3][13]
[15][16]
hTAAR2
[note 3] 		GPR58 Golf, other G protein coupling unknown[note 4] CNS: brain (restricted)[note 5] 
Periphery: olfactory epithelium, intestines, heart, testes, leukocytes 		Template:BullPeriphery: leukocyte chemotaxis
Template:BullOlfaction: chemoreceptor for volatile odorants[note 6]
 [9][13]
[15][16]
[17][18]
TAAR3 GPR57 N/A N/A Pseudogene in humans – N/A N/A [12][13]
[15]
TAAR4 TA2 N/A N/A Pseudogene in humans – N/A N/A [12][13]
[15]
hTAAR5 PNR Gs, Golf,
Gq, G12/13 		CNS: brain (restricted),
spinal cord
Periphery: olfactory epithelium, intestines, testes, leukocytes 		Template:BullOlfaction: chemoreceptor for volatile & foul odorants[note 6] Template:BullAgonists: trimethylamine, N,N-DMEA
Template:BullInverse agonists: 3-iodothyronamine 		[9][13]
[15][20]
[21][22]
[23]
hTAAR6 TA4
TAR4 		Golf, other G protein coupling unknown CNS: brain
Periphery: olfactory epithelium, intestines, testes, leukocytes, kidneys 		Template:BullOlfaction: chemoreceptor for volatile odorants[note 6] Template:BullAgonists: putrescine and cadaverine[24] [9][13]
[15][25]
TAAR7 – N/A N/A Pseudogene in humans – N/A N/A [9][13]
[15]
hTAAR8 TA5
GPR102 		Golf, Gi/o CNS: brain
Periphery: olfactory epithelium, melanocytes,[26] stomach, intestines, heart, testes, leukocytes, kidneys, lungs, muscle, spleen 		Template:BullOlfaction: chemoreceptor for volatile odorants[note 6] Template:BullAgonists: putrescine and cadaverine[24] [9][13]
[15][27]
hTAAR9
[note 7] 		TA3
TAR3 		Golf, other G protein coupling unknown CNS: spinal cord
Periphery: olfactory epithelium, intestines, leukocytes, pituitary gland, skeletal muscle, spleen 		Template:BullOlfaction: chemoreceptor for volatile odorants[note 6] Template:BullAgonist: N-Methyl piperidine (CAS: 626-67-5) [28] [9][13]
[15][29]
Notes

Template:Reflist

Disease links and clinical significance

Ulotaront / SEP 363856 is a TAAR1 agonist in phase 3 clinical trials for schizophrenia and earlier trials for Parkinson's Disease psychosis. The medicine has obtained Breakthrough designation from the US FDA.[30][31][32]Script error: No such module "Unsubst".

See also

References

Template:Reflist

External links

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Template:TAAR ligands Template:G protein-coupled receptors

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    Figure 2: Table of ligands, expression patterns, and species-specific behavioral responses for each TAAR
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