Target Information
Target General Infomation | |||||
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Target ID |
T15571
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Former ID |
TTDR00565
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Target Name |
5-hydroxytryptamine 5A receptor
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Gene Name |
HTR5A
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Synonyms |
5-HT 5A; 5-HT-5; 5-HT-5A; Serotonin receptor; Serotonin receptor 5A; HTR5A
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Target Type |
Research
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Function |
This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activityof this receptor is mediated by G proteins.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T15571
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UniProt ID | |||||
Sequence |
MDLPVNLTSFSLSTPSPLETNHSLGKDDLRPSSPLLSVFGVLILTLLGFLVAATFAWNLL
VLATILRVRTFHRVPHNLVASMAVSDVLVAALVMPLSLVHELSGRRWQLGRRLCQLWIAC DVLCCTASIWNVTAIALDRYWSITRHMEYTLRTRKCVSNVMIALTWALSAVISLAPLLFG WGETYSEGSEECQVSREPSYAVFSTVGAFYLPLCVVLFVYWKIYKAAKFRVGSRKTNSVS PISEAVEVKDSAKQPQMVFTVRHATVTFQPEGDTWREQKEQRAALMVGILIGVFVLCWIP FFLTELISPLCSCDIPAIWKSIFLWLGYSNSFFNPLIYTAFNKNYNSAFKNFFSRQH |
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Inhibitor | (+/-)-nantenine | Drug Info | [530558] | ||
3,4-dihydroquinazolin-2-amine hydrobromide | Drug Info | [529148] | |||
4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
4-methyl-N-propyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529158] | |||
4-propyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
8-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
METHIOTHEPIN | Drug Info | [526655] | |||
N,4-dimethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529158] | |||
N,N-dimethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529148] | |||
N-butyl-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [529158] | |||
SEROTONIN | Drug Info | [529569] | |||
Agonist | 5-CT | Drug Info | [534080] | ||
EMDT | Drug Info | [525722] | |||
lysergic acid | Drug Info | [534080] | |||
TFMPP | Drug Info | [534041] | |||
[125I]LSD | Drug Info | [526046] | |||
[3H]5-CT | Drug Info | [526046] | |||
Antagonist | bufotenine | Drug Info | [534080] | ||
metergoline | Drug Info | [533835] | |||
MPDT | Drug Info | [525722] | |||
SB 699551 | Drug Info | [527628] | |||
SB-699551-A | Drug Info | [536196] | |||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Serotonergic synapse | |||||
PANTHER Pathway | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | ||||
Reactome | Serotonin receptors | ||||
G alpha (i) signalling events | |||||
WikiPathways | Monoamine GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 525722 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8. | ||||
Ref 526046 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. Eur J Pharmacol. 2001 Apr 27;418(3):157-67. | ||||
Ref 526655 | J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). | ||||
Ref 527628 | Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4014-8. | ||||
Ref 529148 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. | ||||
Ref 529158 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):262-6. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. | ||||
Ref 529569 | J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. | ||||
Ref 530558 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. | ||||
Ref 533835 | Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6. | ||||
Ref 534041 | Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. Mol Pharmacol. 1993 Mar;43(3):313-9. |
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