Tachykinin receptor 2

Tachykinin receptor 2
Identifiers
Symbols	TACR2; NK2R; NKNAR; SKR; TAC2R
External IDs	OMIM: 162321 MGI: 98477 HomoloGene: 55548 IUPHAR: NK2 ChEMBL: 2327 GeneCards: TACR2 Gene
Gene Ontology Molecular function • tachykinin receptor activity Cellular component • plasma membrane • integral to plasma membrane Biological process • muscle contraction • tachykinin receptor signaling pathway • excretion Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	6865	21337
Ensembl	ENSG00000075073	ENSMUSG00000020081
UniProt	P21452	P30549
RefSeq (mRNA)	NM_001057	NM_009314
RefSeq (protein)	NP_001048	NP_033340
Location (UCSC)	Chr 10: 71.16 – 71.18 Mb	Chr 10: 62.25 – 62.27 Mb
PubMed search	[1]	[2]

Substance-K receptor is a protein that in humans is encoded by the TACR2 gene.

This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A.

Selective Ligands

Several selective ligands for NK₂ are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant.

Agonists

• GR-64349 - potent and selective agonist, EC₅₀ 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3

Antagonists

• Ibodutant
• Saredutant
• GR-159,897
• MEN-10376 - potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3

See also

• Tachykinin receptor

External links

• "Tachykinin Receptors: NK₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

• Maggi CA, Giuliani S, Patacchini R et al. (1992). "Tachykinin antagonists inhibit nerve-mediated contractions in the circular muscle of the human ileum. Involvement of neurokinin-2 receptors". Gastroenterology 102 (1): 88–96. PMID 1370160. 
• Gerard NP, Gerard C (1991). "Molecular cloning of the human neurokinin-2 receptor cDNA by polymerase chain reaction and isolation of the gene". Ann. N. Y. Acad. Sci. 632: 389–90. doi:10.1111/j.1749-6632.1991.tb33132.x. PMID 1659296. 
• Cyr C, South V, Saltzman A et al. (1991). "Cloning, expression of the human substance K receptor, and analysis of its role in mitogenesis". Ann. N. Y. Acad. Sci. 632: 426–7. doi:10.1111/j.1749-6632.1991.tb33144.x. PMID 1659297. 
• Morten JE, Hopkins B, Powell SJ, Graham A (1992). "Human NK-2 receptor gene maps to chromosome region 10q11-21". Hum. Genet. 88 (2): 200–3. PMID 1661704. 
• Graham A, Hopkins B, Powell SJ et al. (1991). "Isolation and characterisation of the human lung NK-2 receptor gene using rapid amplification of cDNA ends". Biochem. Biophys. Res. Commun. 177 (1): 8–16. doi:10.1016/0006-291X(91)91940-E. PMID 1710456. 
• Gerard NP, Eddy RL, Shows TB, Gerard C (1991). "The human neurokinin A (substance K) receptor. Molecular cloning of the gene, chromosome localization, and isolation of the cDNA from tracheal and gastric tissues". J. Biol. Chem. 266 (2): 1354. PMID 1845990. 
• Kris RM, South V, Saltzman A et al. (1991). "Cloning and expression of the human substance K receptor and analysis of its role in mitogenesis". Cell Growth Differ. 2 (1): 15–22. PMID 1848773. 
• Gerard NP, Eddy RL, Shows TB, Gerard C (1990). "The human neurokinin A (substance K) receptor. Molecular cloning of the gene, chromosome localization, and isolation of cDNA from tracheal and gastric tissues". J. Biol. Chem. 265 (33): 20455–62. PMID 2173708. 
• Alblas J, van Etten I, Khanum A, Moolenaar WH (1995). "C-terminal truncation of the neurokinin-2 receptor causes enhanced and sustained agonist-induced signaling. Role of receptor phosphorylation in signal attenuation". J. Biol. Chem. 270 (15): 8944–51. doi:10.1074/jbc.270.15.8944. PMID 7721803. 
• Bhogal N, Donnelly D, Findlay JB (1994). "The ligand binding site of the neurokinin 2 receptor. Site-directed mutagenesis and identification of neurokinin A binding residues in the human neurokinin 2 receptor". J. Biol. Chem. 269 (44): 27269–74. PMID 7961636. 
• Arkinstall S, Emergy I, Church D et al. (1994). "Calcium influx and protein kinase C alpha activation mediate arachidonic acid mobilization by the human NK-2 receptor expressed in Chinese hamster ovary cells". FEBS Lett. 338 (1): 75–80. doi:10.1016/0014-5793(94)80119-3. PMID 8307161. 
• Brunelleschi S, Bordin G, Colangelo D, Viano I (1999). "Tachykinin receptors on human monocytes: their involvement in rheumatoid arthritis". Neuropeptides 32 (3): 215–23. doi:10.1016/S0143-4179(98)90040-3. PMID 10189055. 
• Patacchini R, Giuliani S, Turini A et al. (2000). "Effect of nepadutant at tachykinin NK(2) receptors in human intestine and urinary bladder". Eur. J. Pharmacol. 398 (3): 389–97. doi:10.1016/S0014-2999(00)00346-0. PMID 10862829. 
• Bellucci F, Carini F, Catalani C et al. (2002). "Pharmacological profile of the novel mammalian tachykinin, hemokinin 1". Br. J. Pharmacol. 135 (1): 266–74. doi:10.1038/sj.bjp.0704443. PMC 1573107. PMID 11786503. 
• Patacchini R, Barbagli G, Palminteri E et al. (2002). "Tachykinin NK1 and NK2 receptors mediate inhibitory vs excitatory motor responses in human isolated corpus cavernosum and spongiosum". Br. J. Pharmacol. 135 (6): 1351–4. doi:10.1038/sj.bjp.0704650. PMC 1573278. PMID 11906947. 
• Candenas ML, Cintado CG, Pennefather JN et al. (2002). "Identification of a tachykinin NK(2) receptor splice variant and its expression in human and rat tissues". Life Sci. 72 (3): 269–77. doi:10.1016/S0024-3205(02)02240-3. PMID 12427486. 
• Strausberg RL, Feingold EA, Grouse LH et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932. 
• Bandari PS, Qian J, Oh HS et al. (2003). "Crosstalk between neurokinin receptors is relevant to hematopoietic regulation: cloning and characterization of neurokinin-2 promoter". J. Neuroimmunol. 138 (1–2): 65–75. doi:10.1016/S0165-5728(03)00096-1. PMID 12742655. 
• Zhao A, Shea-Donohue T (2003). "PAR-2 agonists induce contraction of murine small intestine through neurokinin receptors". Am. J. Physiol. Gastrointest. Liver Physiol. 285 (4): G696–703. doi:10.1152/ajpgi.00064.2003. PMID 12801882. 
• Ota T, Suzuki Y, Nishikawa T et al. (2004). "Complete sequencing and characterization of 21,243 full-length human cDNAs". Nat. Genet. 36 (1): 40–5. doi:10.1038/ng1285. PMID 14702039. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.