Target Information
| 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 1 | 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 2 | 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 3 | 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 4 | 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 5 | 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 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 | 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 9 | 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 10 | Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6. | ||||
| REF 11 | 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 12 | 5-ht5A receptors as a therapeutic target. Pharmacol Ther. 2006 Sep;111(3):707-14. Epub 2006 Mar 6. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.