NK1R, active

Background Information:

The neurokinin‑1 receptor (NK1R) is a class A G protein–coupled receptor that mediates tachykinin signaling and is primarily activated by the neuropeptide substance P. Upon activation, NK1R engages Gq‑family G proteins, leading to phospholipase C activation and intracellular calcium elevation, and can also couple to Gs, reflecting its documented G‑protein promiscuity. Through these signaling pathways, NK1R contributes to key physiological functions including pain transmission, neurogenic inflammation, nausea, and pruritus, and is expressed widely across the central and peripheral nervous systems, smooth muscle, endothelial cells, and immune cells.
Because of its involvement in these processes, NK1R is an important therapeutic target for small‑molecule antagonists. Clinically approved NK1R antagonists, such as aprepitant and netupitant, are widely used for the treatment of chemotherapy‑induced nausea and vomiting. Research also implicates NK1R in depression, inflammation, and other pathological conditions, expanding interest in its role across neurological, gastrointestinal, and immune‑related disease pathways.
This recombinant product is a full-length human NK1R expressed in HEK293F cells, enabling appropriate post-translational modifications and proper membrane integration required for native receptor structure and function. The receptor is purified under native conditions using StrepTactin affinity chromatography followed by size-exclusion chromatography to generate a highly purified and structurally intact preparation. It is maintained in a detergent system containing DDM and CHS, which preserves membrane protein stability and native conformation and is compatible with biochemical assays, receptor reconstitution, and structural studies including cryo-EM. Functional activity is confirmed through ligand-binding assays with aprepitant, demonstrating correct receptor folding and pharmacological relevance.

Target Class:

GPCR

Sub Family:

Class A

Protein Name:

NK1R

Protein Aliases:

TAC1R, SPR, NK-1R

Accession Number:

M76675.1

UniProt Number:

P25103

Gene Name:

TACR1

Gene ID:

6869

Gene Aliases:

SPR; NK1R; NKIR; TAC1R

Target Species:

Human