Target Information

Target General Infomation
Target ID
T58940
Former ID
TTDC00009
Target Name
5-hydroxy-tryptamine 3B receptor
Gene Name
HTR3B
Synonyms
5-HT-3B; 5-HT3B; 5-hydroxytryptamine receptor 3B; Serotonin receptor 3B; HTR3B
Target Type
Discontinued
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. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
BioChemical Class
Neurotransmitter-gated ion-channel
Target Validation
T58940
UniProt ID
O95264
Sequence
MLSSVMAPLWACILVAAGILATDTHHPQDSALYHLSKQLLQKYHKEVRPVYNWTKATTVY
LDLFVHAILDVDAENQILKTSVWYQEVWNDEFLSWNSSMFDEIREISLPLSAIWAPDIII
NEFVDIERYPDLPYVYVNSSGTIENYKPIQVVSACSLETYAFPFDVQNCSLTFKSILHTV
EDVDLAFLRSPEDIQHDKKAFLNDSEWELLSVSSTYSILQSSAGGFAQIQFNVVMRRHPL
VYVVSLLIPSIFLMLVDLGSFYLPPNCRARIVFKTSVLVGYTVFRVNMSNQVPRSVGSTP
LIGHFFTICMAFLVLSLAKSIVLVKFLHDEQRGGQEQPFLCLRGDTDADRPRVEPRAQRA
VVTESSLYGEHLAQPGTLKEVWSQLQSISNYLQTQDQTDQQEAEWLVLLSRFDRLLFQSY
LFMLGIYTITLCSLWALWGGV
Drugs and Mode of Action
Drug(s) BEMESETRON Drug Info Discontinued in Phase 3 Discovery agent [544703]
Inhibitor 2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole Drug Info [532034]
2-(4-Benzyl-piperazin-1-yl)-benzothiazole Drug Info [533917]
2-(4-Methyl-piperazin-1-yl)-quinoline Drug Info [525484]
3-(2-Amino-ethyl)-2-methyl-1H-indol-5-ol Drug Info [532034]
6-(4-Methyl-piperazin-1-yl)-phenanthridine Drug Info [525484]
BEMESETRON Drug Info [528702]
BRL-24682 Drug Info [526544]
MESULERGINE Drug Info [534503]
QUIPAZINE Drug Info [525484]
SEROTONIN Drug Info [525484]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Serotonergic synapse
PANTHER Pathway 5HT3 type receptor mediated signaling pathway
Reactome Ligand-gated ion channel transport
WikiPathways Iron uptake and transport
References
Ref 544703Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000675)
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 526544J Med Chem. 2003 Feb 27;46(5):702-15.Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
Ref 528702J Med Chem. 1992 Jan 24;35(2):310-9.Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships.
Ref 532034J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
Ref 533917J Med Chem. 1994 Apr 29;37(9):1320-5.Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
Ref 534503J Med Chem. 1997 Oct 24;40(22):3670-8.Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.

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