TACR1 (NK1R)/NFAT Luciferase Reporter HEK293 Cell Line

TACR1 (NK1R)/NFAT Luciferase Reporter HEK293 Cell Line is a HEK293 cell line stably expressing full-length human Tachykinin Receptor 1 (TACR1, also known as neurokinin receptor NK1R, accession number: NM_001058.3), and a firefly luciferase reporter under the control of NFAT (nuclear factor of activated T cells) response element. This cell line was validated for its responses to Tachykinin Receptor 1 ligand (Substance P), selective agonist GR73632, and selective antagonist Aprepitant.Figure 1: Illustration of the mechanism by which the luciferase reporter is activated is response to TACR1 agonists.Interested in having us perform the screening and profiling of inhibitors or blocking antibodies? Visit our Cell Signaling Pathway Screening. Tachykinins are a family of neuropeptides that act as neurotransmitters and signaling molecules, regulating pain transmission, inflammation, smooth muscle contraction, and neuroimmune responses. The best-characterized tachykinins, including substance P, neurokinin A, and neurokinin B, exert their effects by binding to neurokinin receptors (NK1R, NK2R, and NK3R) expressed in the nervous, immune, and cardiovascular systems. Neurokinin receptors belong to the family of G protein-coupled receptors (GPCR). Neurokinin receptors couple to G-proteins Gq/11 and Galphas, activating the PLC-Gq signaling pathway and triggering a spike in intracellular calcium Ca2+. Neurokinins play a role in smooth muscle contraction, secretion, proliferation, and nociception. They also contribute to inflammatory bowel disease (IBD), rheumatoid arthritis (RA), multiple sclerosis (MS), psoriasis, and cancer. FDA-approved NKR1 antagonist Aprepitant is used clinically for the treatment of chemotherapy-induced nausea, as NK1R influences the activity of the brain stem emesis centers. More recently, SP and NK1R have gained attention for their role in complex psychiatric processes including stress, anxiety, depression and alcohol addiction.