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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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HTR5A
5-hydroxytryptamine receptor 5A
Chromosome 7 · 7q36.2
NCBI Gene: 3361Ensembl: ENSG00000157219.5HGNC: HGNC:5300UniProt: A4D2N2
49PubMed Papers
20Diseases
5Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
Gi/o-coupled serotonin receptor activityG protein-coupled serotonin receptor activityadenylate cyclase-inhibiting serotonin receptor signaling pathwayprotein bindingschizophreniamajor depressive disorderpost operative nausea and vomitingobesity
✦AI Summary

HTR5A encodes a G-protein coupled receptor for serotonin (5-hydroxytryptamine) and ergot alkaloid derivatives 123. The receptor is coupled to G(i)/G(o) alpha proteins and mediates inhibitory neurotransmission by suppressing adenylate cyclase activity and activating phosphatidylinositol-calcium second messenger systems that regulate intracellular calcium release 123. HTR5A plays roles in multiple neuropsychiatric conditions. Genetic variants in HTR5A are associated with schizophrenia susceptibility and impaired executive function; specifically, rs1800883 showed significant associations with schizophrenia in both discovery and replication cohorts and interacted with perseverative errors on cognitive testing 4. HTR5A variants also contribute to mood disorder etiology through main genetic effects independent of childhood adversity 5. Beyond neuropsychiatry, cortisol upregulates HTR5A expression in adipocytes and macrophages, where it mediates stress-enhanced adipogenesis and metabolic dysfunction 6. HTR5A expression increases in pyramidal neurons in response to increased intracranial pressure, suggesting neuroprotective involvement 7. Placental HTR5A expression patterns are associated with early infant neurodevelopmental outcomes, highlighting serotonergic signaling importance in fetal brain development 8. However, HTR5A polymorphisms did not predict antidepressant treatment response in major depression 9.

Sources cited
1
HTR5A is a G-protein coupled receptor for serotonin mediating inhibitory neurotransmission through G(i)/G(o) coupling
PMID: 35610220
2
HTR5A functions as receptor for serotonin and ergot alkaloids; ligand binding triggers G protein signaling and modulates adenylate cyclase and calcium second messenger systems
PMID: 35835867
3
HTR5A couples to G(i)/G(o) proteins and inhibits adenylate cyclase while activating phosphatidylinositol-calcium signaling
PMID: 9865521
4
HTR5A variant rs1800883 is associated with schizophrenia in both discovery and replication samples and interacts with executive function deficits
PMID: 27897266
5
HTR5A variation (rs1657268) contributes to mood disorder diathesis through main genetic effects independent of childhood adversity
PMID: 19381154
6
Cortisol upregulates HTR5A expression in adipocytes and macrophages where it mediates stress-enhanced adipogenesis
PMID: 30097291
7
HTR5A mRNA expression increases in pyramidal neurons in response to increased intracranial pressure
PMID: 27487831
8
Placental HTR5A expression patterns are associated with early infant neurodevelopmental outcomes
PMID: 41488142
9
HTR5A polymorphisms did not predict escitalopram treatment response in major depression
PMID: 24903772
Disease Associationsⓘ20
schizophreniaOpen Targets
0.59Moderate
major depressive disorderOpen Targets
0.49Moderate
post operative nausea and vomitingOpen Targets
0.48Moderate
obesityOpen Targets
0.46Moderate
depressive disorderOpen Targets
0.38Weak
psychosisOpen Targets
0.37Weak
Nausea and vomitingOpen Targets
0.37Weak
corneal degenerationOpen Targets
0.31Weak
alcohol drinkingOpen Targets
0.30Weak
cervical carcinomaOpen Targets
0.25Weak
Abnormal nasolacrimal system morphologyOpen Targets
0.14Weak
respiratory system neoplasmOpen Targets
0.11Weak
prostate cancerOpen Targets
0.11Weak
Familial prostate cancerOpen Targets
0.11Weak
Follicular CystOpen Targets
0.10Weak
VitiligoOpen Targets
0.08Suggestive
bipolar disorderOpen Targets
0.08Suggestive
Chemotherapy-induced nausea and vomitingOpen Targets
0.07Suggestive
attention deficit hyperactivity disorderOpen Targets
0.07Suggestive
intelligenceOpen Targets
0.07Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets5
AMISULPRIDEApproved
Serotonin (5-HT) receptor antagonist
Nausea and vomiting
DEXFENFLURAMINEApproved
Serotonin (5-HT) receptor agonist
obesity
DEXFENFLURAMINE HYDROCHLORIDEUNKNOWN
Serotonin (5-HT) receptor agonist
ZIMELDINEApproved
Serotonin (5-HT) receptor antagonist
major depressive disorder
ZIMELDINE HYDROCHLORIDEUNKNOWN
Serotonin (5-HT) receptor antagonist
Related Genes
GNALProtein interaction98%GNASProtein interaction97%GNG12Protein interaction89%GNG2Protein interaction85%GNAI1Protein interaction82%OPALINProtein interaction82%
Tissue Expression6 tissues
Brain
100%
Bone Marrow
1%
Liver
0%
Heart
0%
Ovary
0%
Lung
0%
Gene Interaction Network
Click a node to explore
HTR5AGNALGNASGNG12GNG2GNAI1OPALIN
PROTEIN STRUCTURE
Preparing viewer…
PDB7UM5 · 2.73 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.20LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.83 [0.59–1.20]
RankingsWhere HTR5A stands among ~20K protein-coding genes
  • #8,956of 20,598
    Most Researched49
  • #482of 1,025
    FDA-Approved Drug Targets3
  • #12,574of 17,882
    Most Constrained (LOEUF)1.20
Genes detectedHTR5A
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Evaluation of association of common variants in HTR1A and HTR5A with schizophrenia and executive function.
PMID: 27897266
Sci Rep · 2016
1.00
2
Cortisol regulates immune and metabolic processes in murine adipocytes and macrophages through HTR2c and HTR5a serotonin receptors.
PMID: 30097291
Eur J Cell Biol · 2018
0.90
3
Serotonin-related polymorphisms in TPH1 and HTR5A genes are not associated with escitalopram treatment response in Korean patients with major depression.
PMID: 24903772
Neuropsychobiology · 2014
0.80
4
Human neuronal changes in brain edema and increased intracranial pressure.
PMID: 27487831
Acta Neuropathol Commun · 2016
0.70
5
Assignment of the 5-hydroxytryptamine (serotonin) receptor 5A gene (HTR5A) to human chromosome band 7q36.1.
PMID: 8978771
Cytogenet Cell Genet · 1996
0.60