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Target intelligence / Profile preview
Neurokinin 1 Receptor (NK1R)
- Target
- NK1R
- Molecular classification
- G protein-coupled receptor
01
Overview
The neurokinin 1 receptor (NK1R) is a G protein-coupled receptor (GPCR) that primarily binds the neuropeptide substance P, but also interacts with other tachykinins such as neurokinins A and B. It is widely expressed in both the central and peripheral nervous systems, as well as in various non-neuronal tissues including immune cells, muscle, endothelial cells, and exocrine glands. NK1R plays roles in pain transmission, inflammation, and other physiological processes. Antagonists like aprepitant and netupitant are used for chemotherapy-induced nausea and vomiting.
- Other names
- Substance P receptorSPRTachykinin receptor 1TACR1
02
Mechanism of action
NK1R antagonists induce long-lasting conformational changes that block substance P from activating the receptor.
03
Biological functions
Signal transductionPain transmissionInflammation mediationExocrine gland secretionEndocrine secretion modulationVasodilationConnective tissue cell proliferationNeuroimmune modulation
04
Disease associations
InflammationPain perception/transmissionDepressionPruritusAsthma
05
Interacting drugs
Substance P
6 more in the full profile.
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