Tachykinin receptor 2

Tachykinin receptor 2, also known as TACR2, is a human gene.cite web | title = Entrez Gene: TACR2 tachykinin receptor 2| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6865| accessdate = ]

PBB_Summary
section_title =
summary_text = 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.cite web | title = Entrez Gene: TACR2 tachykinin receptor 2| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6865| accessdate = ]

elective 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

* Saredutant
* GR-159,897 - non-peptide antagonist, orally active and anxiolytic "in vivo", 5-Fluoro-3- [2- [4-methoxy-4-( [(R)-phenylsulphinyl] methyl)-1-piperidinyl] ethyl] -1H-indole, CAS# 158848-32-9
* MEN-10376 - potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3

ee also

* Tachykinin receptor

References

Further reading

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

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