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Neurokinin Receptor 1 (NK₁R)
- Target
- NK₁R
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The neurokinin 1 receptor (NK₁R), also known as tachykinin receptor 1 (TACR1) or substance P receptor (SPR), is a G protein-coupled receptor (GPCR) primarily recognized for binding the neuropeptide substance P, its main endogenous ligand. NK₁R is widely expressed in both central and peripheral nervous systems as well as in non-neuronal tissues, mediating diverse biological processes like pain transmission, neurogenic inflammation, emesis, mood regulation, and cell proliferation. Alterations or dysregulation of NK₁ signaling are implicated in various pathologies, including depression, chronic pain, cancer, and chemotherapy-induced nausea/vomiting. NK₁ antagonists, such as aprepitant and netupitant, are clinically used to prevent CINV and are under investigation for other therapeutic applications.
- Other names
- Tachykinin receptor 1TACR1Substance P receptorSPR
02
Mechanism of action
NK₁ receptor antagonist
03
Biological functions
Pain transmissionNeurogenic inflammationEmesis controlMood regulationCell proliferationCell survivalVasodilationVasoconstrictionEndocrine/Paracrine secretion
04
Disease associations
DepressionStress-related disordersAlcohol addictionMigraineChronic pain syndromesInflammatory bowel diseasePruritusViral/bacterial infectionsCancer progressionCancer metastasisChemotherapy-induced nausea/vomitingRadiotherapy-induced emesis
05
Interacting drugs
Aprepitant
1 more in the full profile.
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