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GeneE
26 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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HTR1B
5-hydroxytryptamine receptor 1B
Chromosome 6 · 6q14.1
NCBI Gene: 3351Ensembl: ENSG00000135312.7HGNC: HGNC:5287UniProt: A8K215
219PubMed Papers
20Diseases
24Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
G protein-coupled serotonin receptor activityprotein bindingcellular response to alkaloidcellular response to xenobiotic stimulusmigraine disorderschizophreniamajor depressive disorderpost operative nausea and vomiting
✦AI Summary

HTR1B encodes the 5-hydroxytryptamine receptor 1B, a G-protein coupled receptor that binds serotonin and mediates inhibitory neurotransmission through Gi/Go protein coupling and adenylate cyclase inhibition 1. The receptor regulates the release of serotonin, dopamine, and acetylcholine in the brain, affecting neural activity, pain perception, mood, and behavior 2. HTR1B also plays a role in cerebral artery vasoconstriction 3. Multiple polymorphisms in HTR1B have been identified with functional significance, particularly the -161A>T and G861C variants 4. Meta-analysis evidence supports associations between HTR1B variants and substance use disorders, including alcohol, cocaine, and heroin dependence 5. The gene shows significant associations with attention-deficit/hyperactivity disorder (ADHD), ranking among seven genes with statistically significant pooled evidence across multiple studies 6. HTR1B expression is regulated by its 3' region, which contains regulatory elements that can enhance or suppress gene expression 7. Recent research demonstrates HTR1B's role in opioid use disorder through epigenetic mechanisms, with the rs6296 polymorphism affecting both gene methylation and expression 8. Additionally, HTR1B in osteoblasts contributes to acute myeloid leukemia progression through kynurenine signaling pathways 9.

Sources cited
1
HTR1B is a G-protein coupled serotonin receptor that inhibits adenylate cyclase
PMID: 10452531
2
HTR1B regulates neurotransmitter release affecting neural activity, pain, mood and behavior
PMID: 18476671
3
HTR1B plays a role in cerebral artery vasoconstriction
PMID: 15853772
4
Multiple functional HTR1B polymorphisms identified including -161A>T and G861C variants
PMID: 12437478
5
Meta-analysis shows HTR1B associations with substance use disorders
PMID: 23335468
6
HTR1B shows significant association with ADHD across multiple studies
PMID: 15950004
7
HTR1B 3' region contains regulatory elements affecting gene expression
PMID: 32689951
8
HTR1B rs6296 polymorphism associated with opioid use disorder through methylation and expression mechanisms
PMID: 35438303
9
HTR1B in osteoblasts contributes to acute myeloid leukemia progression via kynurenine signaling
PMID: 35046097
Disease Associationsⓘ20
migraine disorderOpen Targets
0.62Moderate
schizophreniaOpen Targets
0.61Moderate
major depressive disorderOpen Targets
0.49Moderate
post operative nausea and vomitingOpen Targets
0.48Moderate
cardiovascular diseaseOpen Targets
0.47Moderate
obesityOpen Targets
0.47Moderate
mathematical abilityOpen Targets
0.46Moderate
smoking initiationOpen Targets
0.42Moderate
depressive disorderOpen Targets
0.40Weak
Alzheimer diseaseOpen Targets
0.38Weak
psychosisOpen Targets
0.37Weak
Nausea and vomitingOpen Targets
0.37Weak
migraine with auraOpen Targets
0.36Weak
migraine without auraOpen Targets
0.35Weak
ulcerative colitisOpen Targets
0.25Weak
response to antihypertensive drugOpen Targets
0.25Weak
Abruptio PlacentaeOpen Targets
0.20Weak
atrial heart septal defectOpen Targets
0.19Weak
nervous system diseaseOpen Targets
0.19Weak
color vision disorderOpen Targets
0.19Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets24
ALMOTRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
ALMOTRIPTAN MALATEApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
AMISULPRIDEApproved
Serotonin (5-HT) receptor antagonist
Nausea and vomiting
DEXFENFLURAMINEApproved
Serotonin (5-HT) receptor agonist
obesity
DEXFENFLURAMINE HYDROCHLORIDEUNKNOWN
Serotonin (5-HT) receptor agonist
DONITRIPTANPRECLINICAL
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
ELETRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
ELETRIPTAN HYDROBROMIDEApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
ELZASONANPhase II
Serotonin 1b (5-HT1b) receptor antagonist
major depressive disorder
ELZASONAN HYDROCHLORIDEPhase II
Serotonin 1b (5-HT1b) receptor antagonist
mood disorder
ERGOLOID MESYLATESApproved
Serotonin 1a (5-HT1a) receptor agonist
cardiovascular disease
FROVATRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
FROVATRIPTAN SUCCINATEApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
GSK163090Phase II
Serotonin 1a (5-HT1a) receptor antagonist
anxiety disorder
NARATRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
NARATRIPTAN HYDROCHLORIDEApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
RIZATRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
RIZATRIPTAN BENZOATEApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
SUMATRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
SUMATRIPTAN SUCCINATEApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
TRELANSERINPhase II
Serotonin 1b (5-HT1b) receptor antagonist
cardiovascular disease
ZIMELDINEApproved
Serotonin (5-HT) receptor antagonist
major depressive disorder
ZIMELDINE HYDROCHLORIDEUNKNOWN
Serotonin (5-HT) receptor antagonist
ZOLMITRIPTANApproved
Serotonin 1b (5-HT1b) receptor agonist
migraine disorder
Related Genes
GNG4Protein interaction100%GNG2Protein interaction100%GNG7Protein interaction100%TPH2Protein interaction96%SLC6A4Protein interaction95%GNAI2Protein interaction95%
Tissue Expression6 tissues
Brain
100%
Lung
76%
Bone Marrow
58%
Ovary
52%
Liver
3%
Heart
0%
Gene Interaction Network
Click a node to explore
HTR1BGNG4GNG2GNG7TPH2SLC6A4GNAI2
PROTEIN STRUCTURE
Preparing viewer…
PDB4IAR · 2.70 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.72LoF Tolerant
pLIⓘ
0.13Tolerant
Observed/Expected LoF0.44 [0.28–0.72]
RankingsWhere HTR1B stands among ~20K protein-coding genes
  • #1,877of 20,598
    Most Researched219 · top 10%
  • #89of 1,025
    FDA-Approved Drug Targets17 · top 10%
  • #5,533of 17,882
    Most Constrained (LOEUF)0.72
Genes detectedHTR1B
Sources retrieved26 papers
Response time—
📄 Sources
26▼
1
Molecular genetics of attention-deficit/hyperactivity disorder.
PMID: 15950004
Biol Psychiatry · 2005
1.00
2
DNA variation and psychopharmacology of the human serotonin receptor 1B (HTR1B) gene.
PMID: 12437478
Pharmacogenomics · 2002
0.90
3
Attention-deficit/hyperactive disorder updates.
PMID: 36211978
Front Mol Neurosci · 2022
0.80
4
HTR1B genotype and psychopathy: Main effect and interaction with paternal maltreatment.
PMID: 35853382
Psychoneuroendocrinology · 2022
0.76
5
Associations of the 5-hydroxytryptamine (serotonin) receptor 1B gene (HTR1B) with alcohol, cocaine, and heroin abuse.
PMID: 23335468
Am J Med Genet B Neuropsychiatr Genet · 2013
0.70