Tachykinin receptor 1

The tachykinin receptor 1 (TACR1) also known as neurokinin 1 receptor (NK1R) or substance P receptor (SPR) is a G protein coupled receptor found in the central nervous system and peripheral nervous system. The endogenous ligand for this receptor is Substance P, although it has some affinity for other tachykinins. The protein is the product of the TACR1 gene.2KSB, 2KS9, 2KSA686921336ENSG00000115353ENSMUSG00000030043P25103P30548NM_015727NM_001058NM_009313NP_001049NP_056542NP_033339Tachykinins are a family of neuropeptides that share the same hydrophobic C-terminal region with the amino acid sequence Phe-X-Gly-Leu-Met-NH2, where X represents a hydrophobic residue that is either an aromatic or a beta-branched aliphatic. The N-terminal region varies between different tachykinins. The term tachykinin originates in the rapid onset of action caused by the peptides in smooth muscles. Substance P (SP) is the most researched and potent member of the tachykinin family. It is an undecapeptide with the amino acid sequence Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2. SP binds to all three of the tachykinin receptors, but it binds most strongly to the NK1 receptor.This receptor is considered an attractive drug target, particularly with regards to potential analgesics and anti-depressants. It is also a potential treatment for alcoholism and opioid addiction. In addition, it has been identified as a candidate in the etiology of bipolar disorder. Finally NK1R antagonists may also have a role as novel antiemetics and hypnotics.Many selective ligands for NK1 are now available, several of which have gone into clinical use as antiemetics.