Target General Infomation
Target ID
T15571
Former ID
TTDR00565
Target Name
5-hydroxytryptamine 5A receptor
Gene Name
HTR5A
Synonyms
5-HT 5A; 5-HT-5; 5-HT-5A; Serotonin receptor; Serotonin receptor 5A; HTR5A
Target Type
Research
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T15571
UniProt ID
Sequence
MDLPVNLTSFSLSTPSPLETNHSLGKDDLRPSSPLLSVFGVLILTLLGFLVAATFAWNLL
VLATILRVRTFHRVPHNLVASMAVSDVLVAALVMPLSLVHELSGRRWQLGRRLCQLWIAC
DVLCCTASIWNVTAIALDRYWSITRHMEYTLRTRKCVSNVMIALTWALSAVISLAPLLFG
WGETYSEGSEECQVSREPSYAVFSTVGAFYLPLCVVLFVYWKIYKAAKFRVGSRKTNSVS
PISEAVEVKDSAKQPQMVFTVRHATVTFQPEGDTWREQKEQRAALMVGILIGVFVLCWIP
FFLTELISPLCSCDIPAIWKSIFLWLGYSNSFFNPLIYTAFNKNYNSAFKNFFSRQH
Inhibitor (+/-)-nantenine Drug Info [1]
3,4-dihydroquinazolin-2-amine hydrobromide Drug Info [2]
4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [2]
4-methyl-N-propyl-3,4-dihydroquinazolin-2-amine Drug Info [3]
4-propyl-3,4-dihydroquinazolin-2-amine Drug Info [2]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [2]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [2]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [2]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [2]
8-chloro-3,4-dihydroquinazolin-2-amine Drug Info [2]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [2]
METHIOTHEPIN Drug Info [4]
N,4-dimethyl-3,4-dihydroquinazolin-2-amine Drug Info [3]
N,N-dimethyl-3,4-dihydroquinazolin-2-amine Drug Info [2]
N-butyl-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [3]
SEROTONIN Drug Info [5]
Agonist 5-CT Drug Info [6]
EMDT Drug Info [7]
lysergic acid Drug Info [6]
TFMPP Drug Info [8]
[125I]LSD Drug Info [9]
[3H]5-CT Drug Info [9]
Antagonist bufotenine Drug Info [6]
metergoline Drug Info [10]
MPDT Drug Info [7]
SB 699551 Drug Info [11]
SB-699551-A Drug Info [12]
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 1Bioorg 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 2Bioorg 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 3Bioorg 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 4J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
REF 5J 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 6Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization. FEBS Lett. 1995 Dec 27;377(3):451-6.
REF 72-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 8Mouse 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.
REF 9Human 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 10Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6.
REF 11Discovery 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 125-ht5A receptors as a therapeutic target. Pharmacol Ther. 2006 Sep;111(3):707-14. Epub 2006 Mar 6.

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