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Target intelligence / Profile preview
Neurokinin‑1 Receptor (NK‑1R)
- Target
- NK‑1R
- Molecular classification
- G protein-coupled receptor
01
Overview
The Neurokinin-1 Receptor (NK-1R), also known as Tachykinin receptor 1 (TACR1) or Substance P receptor (SPR), is a Class A G protein-coupled receptor (GPCR) that binds to members of the tachykinin family, primarily Substance P. Activation of NK1R mediates diverse physiological processes including pain transmission, inflammation, vasodilation, and emesis. NK1R is coupled to Gq/11 proteins, leading to activation of phospholipase Cβ (PLCB) and increased intracellular calcium levels. Antagonists targeting NK1 receptors, such as aprepitant, are clinically used to treat chemotherapy-induced nausea/vomiting.
- Other names
- Tachykinin receptor 1TACR1Substance P receptorSPR
02
Mechanism of action
Antagonism of substance P binding; inhibition of PLCβ/IP₃/Ca²⁺ signaling pathway
03
Biological functions
Pain transmission (nociception)Inflammation modulationVasodilationEndocrine and paracrine secretionModulation of cell proliferation and survivalHematopoiesisWound healingMicrovasculature permeabilityLeukocyte traffickingNeuromodulation
04
Disease associations
PainInflammationDepressionStressAnxietyEmesis (vomiting)Neurogenic inflammationPsychiatric disorders
05
Interacting drugs
Substance P
3 more in the full profile.
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