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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