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26 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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TACR1
tachykinin receptor 1
Chromosome 2 · 2p12
NCBI Gene: 6869Ensembl: ENSG00000115353.11HGNC: HGNC:11526UniProt: P25103
222PubMed Papers
20Diseases
19Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
RESEARCH IMPACT
Trending
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
protein bindingsperm flagellumtachykinin receptor signaling pathwaysperm headcancerChemotherapy-induced nausea and vomitingNauseapost operative nausea and vomiting
✦AI Summary

TACR1 encodes tachykinin receptor 1 (NK1R), a G protein-coupled receptor that binds substance P with the highest affinity, followed by neurokinin A and neurokinin B 12. Ligand binding triggers dual signaling pathways: phospholipase C activation leading to phosphatidylinositol hydrolysis and increased intracellular calcium, and adenylate cyclase activation increasing cyclic AMP levels. In cancer biology, TACR1 plays a paradoxical role in breast cancer metastasis. Neuronal substance P acts on tumor cell TACR1 to induce death in a TACR1-high cancer subpopulation; the resulting extracellular ssRNAs activate TLR7 on neighboring cells to promote metastatic progression 3. The TACR1 antagonist aprepitant suppresses tumor growth and metastasis, suggesting therapeutic potential 3. In inflammation, TACR1 mediates substance P signaling in vascular endothelial cells. During sleep deprivation-exacerbated periodontitis, substance P from trigeminal neurons increases TACR1-dependent vascular permeability and pro-inflammatory immune cell infiltration; TACR1 antagonism or vascular endothelial TACR1 knockdown alleviates these effects 4. Genetic variation in TACR1 influences clinical phenotypes. TACR1 polymorphisms associate with postoperative nausea/vomiting sex differences 5, alcohol dependence and sensitivity to NK1R antagonist treatment 6, and bipolar disorder, ADHD, and alcohol dependence syndrome 7. Notably, rs3771863 associates with reduced sicca syndrome risk in fibromyalgia patients 8.

Sources cited
1
TACR1 binds substance P with highest affinity, followed by neurokinin A and neurokinin B
PMID: 1718267
2
TACR1 receptor affinity rank order for tachykinins
PMID: 15452552
3
Neuronal substance P acts on tumor TACR1 to promote cancer cell death and metastatic progression through ssRNA-TLR7 axis; TACR1 antagonist aprepitant suppresses metastasis
PMID: 39112700
4
TACR1 mediates substance P effects on vascular permeability and inflammatory cell infiltration in periodontitis; TACR1 antagonism alleviates sleep deprivation-exacerbated periodontitis
PMID: 40489620
5
TACR1 rs3755468 polymorphism associates with postoperative nausea/vomiting with sex-specific effects
PMID: 26012530
6
TACR1 genetic variation and elevated expression in alcohol-preferring rats correlates with NK1R antagonist sensitivity
PMID: 23419547
7
TACR1 polymorphisms associate with bipolar disorder, ADHD, and alcohol dependence syndrome
PMID: 24817687
8
TACR1 rs3771863 polymorphism associates with lower sicca syndrome risk in fibromyalgia patients
PMID: 25786041
Disease Associationsⓘ20
cancerOpen Targets
0.60Moderate
Chemotherapy-induced nausea and vomitingOpen Targets
0.59Moderate
NauseaOpen Targets
0.58Moderate
post operative nausea and vomitingOpen Targets
0.58Moderate
VomitingOpen Targets
0.58Moderate
Nausea and vomitingOpen Targets
0.55Moderate
Hot flashesOpen Targets
0.49Moderate
menopauseOpen Targets
0.48Moderate
neoplasmOpen Targets
0.46Moderate
depressive disorderOpen Targets
0.41Moderate
major depressive disorderOpen Targets
0.41Moderate
breast neoplasmOpen Targets
0.37Weak
atopic eczemaOpen Targets
0.37Weak
prurigo nodularisOpen Targets
0.36Weak
motion sicknessOpen Targets
0.36Weak
PruritusOpen Targets
0.35Weak
gastroparesisOpen Targets
0.34Weak
ovarian dysfunctionOpen Targets
0.33Weak
asthmaOpen Targets
0.32Weak
response to diisocyanateOpen Targets
0.32Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets19
APREPITANTApproved
Neurokinin 1 receptor antagonist
Nausea
BURAPITANTPhase II
Neurokinin 1 receptor antagonist
Urinary incontinence
CASOPITANTApproved
Neurokinin 1 receptor antagonist
Nausea
DNK333Phase II
Neurokinin 1 receptor antagonist
irritable bowel syndrome
ELINZANETANTApproved
Neurokinin 1 receptor antagonist
breast neoplasm
EZLOPITANTPhase II
Neurokinin 1 receptor antagonist
irritable bowel syndrome
FIGOPITANTPhase I
Neurokinin 1 receptor antagonist
FOSAPREPITANTApproved
Neurokinin 1 receptor antagonist
cancer
FOSAPREPITANT DIMEGLUMINEApproved
Neurokinin 1 receptor antagonist
Nausea
FOSNETUPITANTApproved
Neurokinin 1 receptor antagonist
FOSNETUPITANT CHLORIDE HYDROCHLORIDEApproved
Neurokinin 1 receptor antagonist
Chemotherapy-induced nausea and vomiting
NETUPITANTApproved
Neurokinin 1 receptor antagonist
Chemotherapy-induced nausea and vomiting
ORVEPITANTPhase II
Neurokinin 1 receptor antagonist
anxiety disorder
ROLAPITANTApproved
Neurokinin 1 receptor antagonist
Nausea
ROLAPITANT HYDROCHLORIDEApproved
Neurokinin 1 receptor antagonist
Chemotherapy-induced nausea and vomiting
SERLOPITANTPhase III
Neurokinin 1 receptor antagonist
prurigo nodularis
TRADIPITANTPhase III
Neurokinin 1 receptor antagonist
VESTIPITANTPhase II
Neurokinin 1 receptor antagonist
major depressive disorder
VOFOPITANTPhase II
Neurokinin 1 receptor antagonist
post-traumatic stress disorder
Related Genes
UNC80Protein interaction100%GNB1Protein interaction100%GNG2Protein interaction97%SSTProtein interaction94%NTSProtein interaction87%NALCNProtein interaction87%
Tissue Expression6 tissues
Brain
100%
Ovary
85%
Lung
62%
Heart
43%
Liver
10%
Bone Marrow
3%
Gene Interaction Network
Click a node to explore
TACR1UNC80GNB1GNG2SSTNTSNALCN
PROTEIN STRUCTURE
Preparing viewer…
PDB6HLP · 2.20 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.92LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.66 [0.48–0.92]
RankingsWhere TACR1 stands among ~20K protein-coding genes
  • #1,849of 20,598
    Most Researched222 · top 10%
  • #157of 1,025
    FDA-Approved Drug Targets10 · top quartile
  • #8,406of 17,882
    Most Constrained (LOEUF)0.92
Genes detectedTACR1
Sources retrieved26 papers
Response time—
📄 Sources
26▼
1
Neuronal substance P drives metastasis through an extracellular RNA-TLR7 axis.
PMID: 39112700
Nature · 2024
1.00
2
Sleep deficiency exacerbates periodontal inflammation via trigeminal TRPV1 neurons.
PMID: 40489620
Proc Natl Acad Sci U S A · 2025
0.90
3
HBx induces hepatocellular carcinogenesis through ARRB1-mediated autophagy to drive the G
PMID: 33866937
Autophagy · 2021
0.80
4
An intra-brainstem circuitry for pain-induced inhibition of itch.
PMID: 39778623
Neuroscience · 2025
0.76
5
TACR1 gene polymorphism and sex differences in postoperative nausea and vomiting.
PMID: 26012530
Anaesthesia · 2015
0.70