Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTPC4TU)

• DTT Name: 5-HT 3A receptor (HTR3A)
• Synonyms: Serotonin-gated ion channel receptor; Serotonin receptor 3A; HTR3; 5HT3R; 5-hydroxytryptamine receptor 3A; 5-HT3RA; 5-HT3A; 5-HT3-A; 5-HT 3A
• Gene Name: HTR3A
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT3A_HUMAN
• TTD ID: T64591
• Sequence:
  MLLWVQQALLALLLPTLLAQGEARRSRNTTRPALLRLSDYLLTNYRKGVRPVRDWRKPTT
  VSIDVIVYAILNVDEKNQVLTTYIWYRQYWTDEFLQWNPEDFDNITKLSIPTDSIWVPDI
  LINEFVDVGKSPNIPYVYIRHQGEVQNYKPLQVVTACSLDIYNFPFDVQNCSLTFTSWLH
  TIQDINISLWRLPEKVKSDRSVFMNQGEWELLGVLPYFREFSMESSNYYAEMKFYVVIRR
  RPLFYVVSLLLPSIFLMVMDIVGFYLPPNSGERVSFKITLLLGYSVFLIIVSDTLPATAI
  GTPLIGVYFVVCMALLVISLAETIFIVRLVHKQDLQQPVPAWLRHLVLERIAWLLCLREQ
  STSQRPPATSQATKTDDCSAMGNHCSHMGGPQDFEKSPRDRCSPPPPPREASLAVCGLLQ
  ELSSIRQFLEKRDEIREVARDWLRVGSVLDKLLFHIYLLAVLAYSITLVMLWSIWQYA
• 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 in neurons. 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

6 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alosetron	DML2A03	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[2]
Dolasetron	DMMG26Z	Nausea	MD90	Approved	[3]
Levetiracetam	DMTGDN8	Epilepsy	8A60-8A68	Approved	[4]
Palonosetron	DMBHMOX	Nausea	MD90	Approved	[5]
Procaine	DM4LSNE	Anaesthesia	9A78.6	Approved	[1]
Tropisetron	DMNSJ7V	Fibromyalgia	MG30.01	Approved	[4]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cilansetron	DMP0NGX	Irritable bowel syndrome	DD91.0	Phase 3	[6]

5 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	[7]
Norcisapride	DMJSKUI	Gastroesophageal reflux disease	DA22.Z	Discontinued in Phase 2	[8]
YM-114	DML2IXO	Nausea	MD90	Discontinued in Phase 2	[9]
AS-8112	DMIFDPL	Vomiting	MD90	Terminated	[11]
BP4.879a	DMN8FAG	Schizophrenia	6A20	Terminated	[12]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ATI-17000	DMZJVR5	Irritable bowel syndrome	DD91.0	Preclinical	[10]

35 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(4-Quinolin-2-ylpiperazin-1-yl)acetic Acid	DMKF3U6	Discovery agent	N.A.	Investigative	[13]
(S)-zacopride	DM6BON2	Discovery agent	N.A.	Investigative	[14]
1-(biphenyl-4-yl)-3-(4-(piperidin-1-yl)butyl)urea	DM5KZ74	Discovery agent	N.A.	Investigative	[15]
1-phenylbiguanide	DMA4XGL	Discovery agent	N.A.	Investigative	[16]
10,11-dihydro-5H-dibenzo[b,f]azepine	DMS5ICY	Discovery agent	N.A.	Investigative	[17]
2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole	DMCG1HE	Discovery agent	N.A.	Investigative	[18]
2-(4-Benzyl-piperazin-1-yl)-benzothiazole	DM1V7EF	Discovery agent	N.A.	Investigative	[19]
2-(4-Methyl-piperazin-1-yl)-quinoline	DMB8OY6	Discovery agent	N.A.	Investigative	[20]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[21]
3alpha-(1'-Methyl-2'-Indolecarbonyloxy)-tropane	DMCNX34	Discovery agent	N.A.	Investigative	[22]
3alpha-(2'-Indolecarbonyloxy)-nortropane	DM3BRYJ	Discovery agent	N.A.	Investigative	[22]
4-((naphthalen-2-yloxy)methyl)piperidine	DMIQHYZ	Discovery agent	N.A.	Investigative	[23]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[24]
4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane	DMA9DHE	Discovery agent	N.A.	Investigative	[25]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[26]
5-chloro-3,4-dihydroquinazolin-2-amine	DMKEFJ0	Discovery agent	N.A.	Investigative	[26]
5-hydroxyindole	DMI0GMB	Discovery agent	N.A.	Investigative	[27]
6-(4-Methyl-piperazin-1-yl)-phenanthridine	DM1HAWR	Discovery agent	N.A.	Investigative	[20]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile	DM6I5K1	Discovery agent	N.A.	Investigative	[23]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[28]
bilobalide	DM09Z35	Discovery agent	N.A.	Investigative	[29]
BRL-24682	DMSB4EW	Discovery agent	N.A.	Investigative	[30]
CP-810123	DMXDG13	Discovery agent	N.A.	Investigative	[25]
FLUPENTIXOLE	DMELB5S	Discovery agent	N.A.	Investigative	[17]
MESULERGINE	DMKGWAH	Discovery agent	N.A.	Investigative	[31]
meta-chlorphenylbiguanide	DMEA8GP	Discovery agent	N.A.	Investigative	[32]
PH-709829	DM5GY6Z	Discovery agent	N.A.	Investigative	[33]
QUIPAZINE	DMPY6IG	Discovery agent	N.A.	Investigative	[34]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[20]
TMB-8	DMCN2B8	Discovery agent	N.A.	Investigative	[35]
trichloroethanol	DMNALMF	Discovery agent	N.A.	Investigative	[36]
[3H](S)-zacopride	DM0B54M	Discovery agent	N.A.	Investigative	[37]
[3H]GR65630	DMMHSYA	Discovery agent	N.A.	Investigative	[38]
[3H]granisetron	DMB9VGW	Discovery agent	N.A.	Investigative	[39]
[3H]ramosetron	DM21B46	Discovery agent	N.A.	Investigative	[40]

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	6.60E-01	1.08E-02	0.04

References

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