Target General Infomation
Target ID
Former ID
Target Name
5-hydroxytryptamine 5A receptor
Gene Name
5-HT 5A; 5-HT-5; 5-HT-5A; Serotonin receptor; Serotonin receptor 5A; HTR5A
Target Type
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
UniProt ID
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]
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
Ref 5257222-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
Ref 526046Human 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 526655J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
Ref 527628Discovery 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 529148Bioorg 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 529158Bioorg 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 529569J 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 530558Bioorg 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 533835Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6.
Ref 534041Mouse 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 534080Expression 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 5361965-ht5A receptors as a therapeutic target. Pharmacol Ther. 2006 Sep;111(3):707-14. Epub 2006 Mar 6.

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