Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTR6K75)

• DTT Name: 5-HT 3B receptor (HTR3B)
• Synonyms: Serotonin receptor 3B; 5-hydroxytryptamine receptor 3B; 5-HT3B; 5-HT3-B; 5-HT-3B
• Gene Name: HTR3B
• DTT Type: Discontinued target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT3B_HUMAN
• TTD ID: T58940
• Sequence:
  MLSSVMAPLWACILVAAGILATDTHHPQDSALYHLSKQLLQKYHKEVRPVYNWTKATTVY
  LDLFVHAILDVDAENQILKTSVWYQEVWNDEFLSWNSSMFDEIREISLPLSAIWAPDIII
  NEFVDIERYPDLPYVYVNSSGTIENYKPIQVVSACSLETYAFPFDVQNCSLTFKSILHTV
  EDVDLAFLRSPEDIQHDKKAFLNDSEWELLSVSSTYSILQSSAGGFAQIQFNVVMRRHPL
  VYVVSLLIPSIFLMLVDLGSFYLPPNCRARIVFKTSVLVGYTVFRVNMSNQVPRSVGSTP
  LIGHFFTICMAFLVLSLAKSIVLVKFLHDEQRGGQEQPFLCLRGDTDADRPRVEPRAQRA
  VVTESSLYGEHLAQPGTLKEVWSQLQSISNYLQTQDQTDQQEAEWLVLLSRFDRLLFQSY
  LFMLGIYTITLCSLWALWGGV
• 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.
• KEGG Pathway: Serotonergic synapse (hsa04726)
• Reactome Pathway: Ligand-gated ion channel transport (R-HSA-975298)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BEMESETRON	DMSPJX9	N. A.	N. A.	Discontinued in Phase 3	[1]

15 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(S)-zacopride	DM6BON2	Discovery agent	N.A.	Investigative	[2]
1-phenylbiguanide	DMA4XGL	Discovery agent	N.A.	Investigative	[2]
2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole	DMCG1HE	Discovery agent	N.A.	Investigative	[3]
2-(4-Benzyl-piperazin-1-yl)-benzothiazole	DM1V7EF	Discovery agent	N.A.	Investigative	[4]
2-(4-Methyl-piperazin-1-yl)-quinoline	DMB8OY6	Discovery agent	N.A.	Investigative	[5]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[6]
6-(4-Methyl-piperazin-1-yl)-phenanthridine	DM1HAWR	Discovery agent	N.A.	Investigative	[5]
bilobalide	DM09Z35	Discovery agent	N.A.	Investigative	[7]
BRL-24682	DMSB4EW	Discovery agent	N.A.	Investigative	[8]
MESULERGINE	DMKGWAH	Discovery agent	N.A.	Investigative	[9]
meta-chlorphenylbiguanide	DMEA8GP	Discovery agent	N.A.	Investigative	[2]
QUIPAZINE	DMPY6IG	Discovery agent	N.A.	Investigative	[5]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[5]
trichloroethanol	DMNALMF	Discovery agent	N.A.	Investigative	[10]
[3H]granisetron	DMB9VGW	Discovery agent	N.A.	Investigative	[2]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Irritable bowel syndrome	DD91.0	Rectal colon tissue	3.82E-01	0.04	0.1

References

• [1] Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9.
• [2] Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors. Neuropharmacology. 2001 Aug;41(2):282-4.
• [3] Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. J Med Chem. 1990 Jan;33(1):13-6.
• [4] Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties. J Med Chem. 1994 Apr 29;37(9):1320-5.
• [5] Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy ... J Med Chem. 1999 May 6;42(9):1556-75.
• [6] The 5-HT3B subunit is a major determinant of serotonin-receptor function. Nature. 1999 Jan 28;397(6717):359-63.
• [7] Ginkgolide B and bilobalide block the pore of the 5-HT eceptor at a location that overlaps the picrotoxin binding site. Neuropharmacology. 2011 Feb-Mar;60(2-3):488-95.
• [8] Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotoni... J Med Chem. 2003 Feb 27;46(5):702-15.
• [9] Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. J Med Chem. 1997 Oct 24;40(22):3670-8.
• [10] Co-expression of the 5-HT(3B) subunit with the 5-HT(3A) receptor reduces alcohol sensitivity. Brain Res Mol Brain Res. 2005 Dec 14;142(2):146-50.