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50 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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HTR2A
5-hydroxytryptamine receptor 2A
Chromosome 13 · 13q14.2
NCBI Gene: 3356Ensembl: ENSG00000102468.11HGNC: HGNC:5293UniProt: A0A7P0PKG8
736PubMed Papers
20Diseases
76Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
RESEARCH IMPACT
Highly Studied
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
G protein-coupled serotonin receptor complexintracellular calcium ion homeostasisidentical protein bindingpositive regulation of phosphatidylinositol biosynthetic processmajor depressive disorderschizophreniaautismbipolar disorder
✦AI Summary

HTR2A encodes the 5-hydroxytryptamine receptor 2A, a G protein-coupled serotonin receptor that mediates Gq/11-coupled signaling and intracellular calcium mobilization 1. The receptor binds serotonin and also serves as a target for hallucinogenic compounds like psilocybin and LSD, which activate its active state and mediate both therapeutic and psychoactive effects 1. Mechanistically, HTR2A activates phospholipase C-dependent signaling cascades and regulates excitatory synaptic transmission. Recent evidence demonstrates that HTR2A expression is transcriptionally regulated by Zkscan4 in the hippocampus, with reduced HTR2A expression conferring resilience to chr13 stress 2. Additionally, HTR2A mediates hepatic serotonin signaling via the gut-liver axis, where HTR2A activation promotes high-fat diet-induced hepatic steatosis 3. Clinically, HTR2A genetic variants (particularly rs6313 T102C) show modest associations with substance use disorders, especially alcohol dependence 4. However, current evidence does not support clinical use of HTR2A genotyping for antidepressant dosing 5, and associations with antipsychotic response are ethnicity- and drug-dependent 6. HTR2A's role in other psychiatric disorders remains inconsistently replicated 7. HTR2A antagonism shows therapeutic potential for nonalcoholic fatty liver disease treatment 3.

Sources cited
1
HTR2A is a Gq-coupled serotonin receptor activated by hallucinogens like psilocybin and LSD; activation is key to psychedelic therapeutic and hallucinogenic effects
PMID: 32946782
2
Zkscan4 regulates HTR2A transcription in the hippocampus; reduced HTR2A expression confers resilience to chronic stress-induced depression
PMID: 40408492
3
HTR2A mediates gut-derived serotonin signaling in the liver; HTR2A activation promotes high-fat diet-induced hepatic steatosis; HTR2A antagonism ameliorates NAFLD
PMID: 30446669
4
HTR2A rs6313 variant shows association with alcohol dependence and substance use disorders in meta-analysis
PMID: 24178752
5
Current evidence does not support clinical use of HTR2A genotyping for antidepressant prescribing decisions
PMID: 37032427
6
HTR2A rs6313 polymorphism associations with antipsychotic efficacy are ethnicity- and drug-dependent, with no overall significant association
PMID: 37726709
7
HTR2A variants have been associated with multiple psychiatric disorders, but most studies show conflicting results and evidence of minimal impact
PMID: 17691947
Disease Associationsⓘ20
major depressive disorderOpen Targets
0.70Strong
schizophreniaOpen Targets
0.62Moderate
autismOpen Targets
0.62Moderate
bipolar disorderOpen Targets
0.61Moderate
psychosisOpen Targets
0.61Moderate
depressive disorderOpen Targets
0.60Moderate
bipolar I disorderOpen Targets
0.60Moderate
AgitationOpen Targets
0.60Moderate
aggressive behaviorOpen Targets
0.60Moderate
schizoaffective disorderOpen Targets
0.60Moderate
Tourette syndromeOpen Targets
0.59Moderate
mental or behavioural disorderOpen Targets
0.59Moderate
Parkinson diseaseOpen Targets
0.57Moderate
insomniaOpen Targets
0.57Moderate
autism spectrum disorderOpen Targets
0.52Moderate
Nausea and vomitingOpen Targets
0.51Moderate
conduct disorderOpen Targets
0.51Moderate
Muscle spasmOpen Targets
0.50Moderate
post operative nausea and vomitingOpen Targets
0.49Moderate
obesityOpen Targets
0.47Moderate
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets76
AMISULPRIDEApproved
Serotonin (5-HT) receptor antagonist
Nausea and vomiting
ARIPIPRAZOLEApproved
Serotonin 2a (5-HT2a) receptor antagonist
ARIPIPRAZOLE LAUROXILApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
ASENAPINEApproved
Dopamine D2 receptor antagonist
ASENAPINE MALEATEApproved
Dopamine D2 receptor antagonist
schizophrenia
BLONANSERINApproved
Dopamine D2 receptor antagonist
schizophrenia
BREXPIPRAZOLEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
CARPHENAZINEApproved
Serotonin 2c (5-HT2c) receptor antagonist
insomnia
CHLORPROMAZINEApproved
D2-like dopamine receptor antagonist
Nausea and vomiting
CHLORPROMAZINE HYDROCHLORIDEApproved
D2-like dopamine receptor antagonist
CHLORPROTHIXENEApproved
Dopamine D2 receptor antagonist
mental or behavioural disorder
CLOTHIAPINEApproved
Dopamine D4 receptor antagonist
schizophrenia
CLOZAPINEApproved
Dopamine D2 receptor antagonist
schizophrenia
CYCLOBENZAPRINEApproved
Serotonin 2a (5-HT2a) receptor antagonist
depressive disorder
CYCLOBENZAPRINE HYDROCHLORIDEApproved
Serotonin 2a (5-HT2a) receptor antagonist
spinal cord disease
DEXFENFLURAMINEApproved
Serotonin (5-HT) receptor agonist
obesity
DEXFENFLURAMINE HYDROCHLORIDEUNKNOWN
Serotonin (5-HT) receptor agonist
DROPERIDOLApproved
D2-like dopamine receptor antagonist
Nausea and vomiting
EPLIVANSERINPhase III
Serotonin 2a (5-HT2a) receptor antagonist
insomnia
ESMIRTAZAPINEPhase III
Serotonin 2a (5-HT2a) receptor antagonist
insomnia
ESMIRTAZAPINE MALEATEPhase III
Serotonin 2a (5-HT2a) receptor antagonist
insomnia
HALOPERIDOLApproved
Serotonin 2a (5-HT2a) receptor antagonist
conduct disorder
HALOPERIDOL DECANOATEApproved
D2-like dopamine receptor inverse agonist
HALOPERIDOL LACTATEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
IFERANSERINPhase III
Serotonin 2a (5-HT2a) receptor antagonist
hemorrhoid
ILOPERIDONEApproved
Dopamine D2 receptor antagonist
schizophrenia
LOXAPINEApproved
D2-like dopamine receptor antagonist
Agitation
LOXAPINE SUCCINATEApproved
Serotonin 2a (5-HT2a) receptor antagonist
LUMATEPERONEApproved
Serotonin transporter inhibitor
LURASIDONEApproved
Dopamine D2 receptor antagonist
schizophrenia
LURASIDONE HYDROCHLORIDEApproved
Dopamine D2 receptor antagonist
MESORIDAZINEApproved
Dopamine D2 receptor antagonist
schizophrenia
MINAPRINEApproved
Dopamine D1 and D2 receptor agonist
depressive disorder
MINAPRINE HYDROCHLORIDEUNKNOWN
Dopamine D1 and D2 receptor agonist
MIRTAZAPINEApproved
Serotonin 2a (5-HT2a) receptor antagonist
major depressive disorder
MOLINDONEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
MOLINDONE HYDROCHLORIDEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
NEFAZODONEApproved
Serotonin 2a (5-HT2a) receptor antagonist
major depressive disorder
NEFAZODONE HYDROCHLORIDEApproved
Serotonin 2a (5-HT2a) receptor antagonist
major depressive disorder
NELOTANSERINPhase II
Serotonin 2a (5-HT2a) receptor inverse agonist
Lewy body dementia
OLANZAPINEApproved
D2-like dopamine receptor antagonist
bipolar disorder
OLANZAPINE PAMOATEApproved
D2-like dopamine receptor antagonist
schizophrenia
PALIPERIDONEApproved
Serotonin 2a (5-HT2a) receptor antagonist
PALIPERIDONE PALMITATEApproved
Dopamine D2 receptor antagonist
schizoaffective disorder
PIMAVANSERINApproved
Serotonin 2a (5-HT2a) receptor inverse agonist
Parkinson disease
PIMAVANSERIN TARTRATEApproved
Serotonin 2a (5-HT2a) receptor inverse agonist
Parkinson disease
PIMOZIDEApproved
Dopamine receptor antagonist
Tics
PROMAZINEApproved
D2-like dopamine receptor antagonist
Agitation
PRUVANSERINPhase II
Serotonin 2a (5-HT2a) receptor antagonist
sleep-wake disorder
PSILOCYBINPhase III
Serotonin 2a (5-HT2a) receptor agonist
treatment resistant depression
QUETIAPINEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
QUETIAPINE FUMARATEApproved
Serotonin 2a (5-HT2a) receptor antagonist
bipolar disorder
RISPERIDONEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
SARPOGRELATEApproved
Serotonin 2a (5-HT2a) receptor antagonist
SB-773812Phase II
Dopamine D2 receptor antagonist
schizophrenia
SERTINDOLEApproved
Dopamine D2 receptor antagonist
psychosis
TEDATIOXETINEPhase II
Serotonin 2c (5-HT2c) receptor antagonist
major depressive disorder
TEMANOGRELPhase II
Serotonin 2a (5-HT2a) receptor inverse agonist
THIORIDAZINEApproved
D2-like dopamine receptor antagonist
schizophrenia
THIORIDAZINE HYDROCHLORIDEApproved
D2-like dopamine receptor antagonist
THIOTHIXENEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
TRAZODONEApproved
Serotonin 2a (5-HT2a) receptor antagonist
depressive disorder
TRAZODONE HYDROCHLORIDEApproved
Serotonin 2a (5-HT2a) receptor antagonist
TRELANSERINPhase II
Serotonin 1b (5-HT1b) receptor antagonist
cardiovascular disease
TRIFLUOPERAZINEApproved
D2-like dopamine receptor antagonist
schizophrenia
TRIFLUOPERAZINE HYDROCHLORIDEApproved
D2-like dopamine receptor antagonist
anxiety disorder
TRIMIPRAMINEApproved
Histamine H1 receptor antagonist
major depressive disorder
TRIMIPRAMINE MALEATEApproved
Histamine H1 receptor antagonist
VABICASERINPhase II
Serotonin 2c (5-HT2c) receptor agonist
psychosis
VABICASERIN HYDROCHLORIDEPhase I
Serotonin 2c (5-HT2c) receptor agonist
VOLINANSERINPhase III
Serotonin 2a (5-HT2a) receptor antagonist
sleep-wake disorder
ZIMELDINEApproved
Serotonin (5-HT) receptor antagonist
major depressive disorder
ZIMELDINE HYDROCHLORIDEUNKNOWN
Serotonin (5-HT) receptor antagonist
ZIPRASIDONEApproved
Serotonin 2a (5-HT2a) receptor antagonist
schizophrenia
ZIPRASIDONE HYDROCHLORIDEApproved
Serotonin 2a (5-HT2a) receptor antagonist
bipolar disorder
ZIPRASIDONE MESYLATEApproved
Serotonin 2a (5-HT2a) receptor antagonist
Related Genes
GNB1Protein interaction99%CNR1Protein interaction99%CACNA1CProtein interaction96%CACNA1DProtein interaction96%CACNA1FProtein interaction96%CACNA1SProtein interaction96%
Tissue Expression6 tissues
Brain
100%
Heart
5%
Bone Marrow
5%
Liver
3%
Ovary
2%
Lung
1%
Gene Interaction Network
Click a node to explore
HTR2AGNB1CNR1CACNA1CCACNA1DCACNA1FCACNA1S
PROTEIN STRUCTURE
Preparing viewer…
PDB7WC8 · 2.45 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.63LoF Tolerant
pLIⓘ
0.36Tolerant
Observed/Expected LoF0.40 [0.27–0.63]
RankingsWhere HTR2A stands among ~20K protein-coding genes
  • #286of 20,598
    Most Researched736 · top 5%
  • #13of 1,025
    FDA-Approved Drug Targets59 · top 5%
  • #4,474of 17,882
    Most Constrained (LOEUF)0.63
Genes detectedHTR2A
Sources retrieved50 papers
Response time—
📄 Sources
50▼
1
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6, CYP2C19, CYP2B6, SLC6A4, and HTR2A Genotypes and Serotonin Reuptake Inhibitor Antidepressants.
PMID: 37032427
Clin Pharmacol Ther · 2023
1.00
2
Maternal Metabolic State and Fetal Sex and Genotype Modulate Methylation of the Serotonin Receptor Type 2A Gene (
PMID: 35203678
Biomedicines · 2022
0.90
3
Structure of a Hallucinogen-Activated Gq-Coupled 5-HT
PMID: 32946782
Cell · 2020
0.90
4
[Association of gene polymorphisms DRD3 rs6280, COMT rs4680 and HTR2A rs7322347 with schizophrenia].
PMID: 35904302
Zh Nevrol Psikhiatr Im S S Korsakova · 2022
0.88
5
Genomic structure and expression of the human serotonin 2A receptor gene (HTR2A) locus: identification of novel HTR2A and antisense (HTR2A-AS1) exons.
PMID: 26738766
BMC Genet · 2016
0.80