Target Information
Target General Infomation | |||||
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Target ID |
T99524
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Former ID |
TTDI01906
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Target Name |
Trace amine-associated receptor-1
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Gene Name |
TAAR1
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Synonyms |
TaR-1; Trace amine receptor 1; TAAR1
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Target Type |
Successful
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Disease | Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90] | ||||
Attention deficit disorder with hyperactivity [ICD10: F90] | |||||
Attention deficit hyperactivity disorder; Narcolepsy [ICD10: F90, G47.4] | |||||
Diagnostic evaluation of horner's syndrome [ICD10: G90.2] | |||||
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | |||||
Unspecified [ICD code not available] | |||||
Function |
Receptor for trace amines, including beta- phenylethylamine (b-PEA), p-tyramine (p-TYR), octopamine and tryptamine, with highest affinity for b-PEA and p-TYR. Unresponsive to classical biogenic amines,such as epinephrine and histamine and only partially activated by dopamine and serotonine. Trace amines are biogenic amines present in very low levels in mammalian tissues. Although some trace amineshave clearly defined roles as neurotransmitters in invertebrates, the extent to which they function as true neurotransmitters in vertebrates has remained speculative. Trace amines are likely to be involved in a variety of physiological functions that have yet to be fully understood. The signal transduced by this receptor is mediated by the G(s)-class of G-proteins which activate adenylate cyclase.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | |||||
Sequence |
MMPFCHNIINISCVKNNWSNDVRASLYSLMVLIILTTLVGNLIVIVSISHFKQLHTPTNW
LIHSMATVDFLLGCLVMPYSMVRSAEHCWYFGEVFCKIHTSTDIMLSSASIFHLSFISID RYYAVCDPLRYKAKMNILVICVMIFISWSVPAVFAFGMIFLELNFKGAEEIYYKHVHCRG GCSVFFSKISGVLTFMTSFYIPGSIMLCVYYRIYLIAKEQARLISDANQKLQIGLEMKNG ISQSKERKAVKTLGIVMGVFLICWCPFFICTVMDPFLHYIIPPTLNDVLIWFGYLNSTFN PMVYAFFYPWFRKALKMMLFGKIFQKDSSRCKLFLELSS |
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Drugs and Mode of Action | |||||
Drug(s) | Amphetamine | Drug Info | Approved | Attention deficit disorder with hyperactivity | [551871] |
Dextroamphetamine | Drug Info | Approved | Attention deficit hyperactivity disorder; Narcolepsy | [551871] | |
Hydroxyamphetamine Hydrobromide | Drug Info | Approved | Diagnostic evaluation of horner's syndrome | [551871] | |
Lisdexamfetamine | Drug Info | Approved | Attention deficit hyperactivity disorder | [538579], [542228] | |
NT0202 | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [526471], [526676], [532175], [532852], [551871] | |
SPD-465 | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [526471], [526676], [532175], [532852], [551871] | |
D-amphetamine transdermal | Drug Info | Phase 2 | Attention deficit hyperactivity disorder | [526471], [526676], [532175], [532852], [551871] | |
RG-7351 | Drug Info | Phase 1 | Major depressive disorder | [549026] | |
Amphetamine | Drug Info | Investigative | Attention deficit hyperactivity disorder | [468035], [526471], [526676], [532175], [532852], [551871] | |
Agonist | 3-iodothyronamine | Drug Info | [528833] | ||
NT0202 | Drug Info | [526471], [526676], [532175], [532852], [551871] | |||
R(-)amphetamine | Drug Info | [528610] | |||
RG-7351 | Drug Info | [526471], [526676], [532175], [532852], [551610], [551871] | |||
RO5166017 | Drug Info | [531452] | |||
SPD-465 | Drug Info | [526471], [526676], [532175], [532852], [551871] | |||
tyramine | Drug Info | [531694] | |||
[3H]tyramine | Drug Info | [526105] | |||
Modulator | Amphetamine | Drug Info | [526471], [526676], [532175], [532852], [551871] | ||
D-amphetamine transdermal | Drug Info | [526471], [526676], [532175], [532852], [551871] | |||
Dextroamphetamine | Drug Info | [526471], [526676], [532175], [532852] | |||
dextroamphetamine sulfate (oral liquid, ADHD), Auriga | Drug Info | [526471], [526676], [532175], [532852] | |||
Hydroxyamphetamine Hydrobromide | Drug Info | ||||
Lisdexamfetamine | Drug Info | [529282], [531678] | |||
methamphetamine intravenous | Drug Info | [526471], [526676], [532175], [532852] | |||
PF-08 | Drug Info | [526471], [526676], [532175], [532852], [551871] | |||
Antagonist | EPPTB | Drug Info | [530500] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Reactome | G alpha (s) signalling events | ||||
References | |||||
Ref 468035 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4804). | ||||
Ref 526471 | Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice. Neurosci Lett. 2002 Dec 16;334(3):145-8. | ||||
Ref 526676 | Alpha-1B adrenergic receptor knockout mice are protected against methamphetamine toxicity. J Neurochem. 2003 Jul;86(2):413-21. | ||||
Ref 532175 | Involvement of the alpha(1D)-adrenergic receptor in methamphetamine-induced hyperthermia and neurotoxicity in rats. Neurotox Res. 2013 Aug;24(2):130-8. | ||||
Ref 532852 | Methamphetamine and HIV-1-induced neurotoxicity: role of trace amine associated receptor 1 cAMP signaling in astrocytes. Neuropharmacology. 2014 Oct;85:499-507. | ||||
Ref 538579 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021977. | ||||
Ref 542228 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7213). | ||||
Ref 526105 | Trace amines: identification of a family of mammalian G protein-coupled receptors. Proc Natl Acad Sci U S A. 2001 Jul 31;98(16):8966-71. Epub 2001 Jul 17. | ||||
Ref 526471 | Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice. Neurosci Lett. 2002 Dec 16;334(3):145-8. | ||||
Ref 526676 | Alpha-1B adrenergic receptor knockout mice are protected against methamphetamine toxicity. J Neurochem. 2003 Jul;86(2):413-21. | ||||
Ref 528610 | The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia. Genes Brain Behav. 2007 Oct;6(7):628-39. Epub 2006 Dec 21. | ||||
Ref 528833 | Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1. J Med Chem. 2007 Jun 14;50(12):2787-98. Epub 2007 May 12. | ||||
Ref 530500 | The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6. | ||||
Ref 531452 | TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A. 2011 May 17;108(20):8485-90. | ||||
Ref 531678 | Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class. Bioorg Med Chem. 2011 Dec 1;19(23):7044-8. | ||||
Ref 531694 | Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists. PLoS One. 2011;6(10):e27073. | ||||
Ref 532175 | Involvement of the alpha(1D)-adrenergic receptor in methamphetamine-induced hyperthermia and neurotoxicity in rats. Neurotox Res. 2013 Aug;24(2):130-8. |
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