Target General Infomation
Target ID
T15571 (Former ID: TTDR00565)
Target Name
5-HT 5A receptor (HTR5A)
Synonyms
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
Gene Name
HTR5A
Target Type
Successful target
[1]
Disease [+] 1 Target-related Diseases +
1 Pituitary gland disorder [ICD-11: 5A60-5A61]
Function
The activity of this receptor is mediated by G proteins. 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.
BioChemical Class
GPCR rhodopsin
UniProt ID
5HT5A_HUMAN
Sequence
MDLPVNLTSFSLSTPSPLETNHSLGKDDLRPSSPLLSVFGVLILTLLGFLVAATFAWNLL
VLATILRVRTFHRVPHNLVASMAVSDVLVAALVMPLSLVHELSGRRWQLGRRLCQLWIAC
DVLCCTASIWNVTAIALDRYWSITRHMEYTLRTRKCVSNVMIALTWALSAVISLAPLLFG
WGETYSEGSEECQVSREPSYAVFSTVGAFYLPLCVVLFVYWKIYKAAKFRVGSRKTNSVS
PISEAVEVKDSAKQPQMVFTVRHATVTFQPEGDTWREQKEQRAALMVGILIGVFVLCWIP
FFLTELISPLCSCDIPAIWKSIFLWLGYSNSFFNPLIYTAFNKNYNSAFKNFFSRQH
Drugs and Modes of Action
Approved Drug(s) [+] 1 Approved Drugs +
1 Metergolin Drug Info Approved Hyperprolactinaemia [2]
Mode of Action [+] 3 Modes of Action +
Antagonist [+] 5 Antagonist drugs +
1 Metergolin Drug Info [1]
2 bufotenine Drug Info [6]
3 MPDT Drug Info [7]
4 SB 699551 Drug Info [9]
5 SB-699551-A Drug Info [10]
Inhibitor [+] 16 Inhibitor drugs +
1 (+/-)-nantenine Drug Info [3]
2 3,4-dihydroquinazolin-2-amine hydrobromide Drug Info [4]
3 4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [4]
4 4-methyl-N-propyl-3,4-dihydroquinazolin-2-amine Drug Info [5]
5 4-propyl-3,4-dihydroquinazolin-2-amine Drug Info [4]
6 5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [4]
7 5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [4]
8 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [4]
9 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [4]
10 8-chloro-3,4-dihydroquinazolin-2-amine Drug Info [4]
11 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [4]
12 METHIOTHEPIN Drug Info [8]
13 N,4-dimethyl-3,4-dihydroquinazolin-2-amine Drug Info [5]
14 N,N-dimethyl-3,4-dihydroquinazolin-2-amine Drug Info [4]
15 N-butyl-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [5]
16 SEROTONIN Drug Info [11]
Agonist [+] 6 Agonist drugs +
1 5-CT Drug Info [6]
2 EDMT Drug Info [7]
3 lysergic acid Drug Info [6]
4 TFMPP Drug Info [12]
5 [125I]LSD Drug Info [13]
6 [3H]5-CT Drug Info [13]
Target Affiliated Biological Pathways
KEGG Pathway [+] 3 KEGG Pathways +
1 Calcium signaling pathway
2 Neuroactive ligand-receptor interaction
3 Serotonergic synapse
Panther Pathway [+] 1 Panther Pathways +
1 Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Reactome [+] 2 Reactome Pathways +
1 Serotonin receptors
2 G alpha (i) signalling events
WikiPathways [+] 4 WikiPathways +
1 Monoamine GPCRs
2 GPCRs, Class A Rhodopsin-like
3 GPCR ligand binding
4 GPCR downstream signaling
Target-Related Models and Studies
Target Validation
References
REF 1 Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6.
REF 2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 4 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
REF 5 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. Bioorg Med Chem Lett. 2008 Jan 1;18(1):262-6.
REF 6 Expression 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 7 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 8 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
REF 9 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 10 5-ht5A receptors as a therapeutic target. Pharmacol Ther. 2006 Sep;111(3):707-14.
REF 11 Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
REF 12 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.
REF 13 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.

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