Tachykinin receptor 3

edit

Tachykinin receptor 3
Identifiers
Symbols	TACR3; MGC148060; MGC148061; NK3R; TAC3RL
External IDs	OMIM: 162332 MGI: 892968 HomoloGene: 824 IUPHAR: NK3 GeneCards: TACR3 Gene
Gene Ontology Molecular function • rhodopsin-like receptor activity • receptor activity • tachykinin receptor activity Cellular component • plasma membrane • integral to plasma membrane Biological process • signal transduction • tachykinin signaling pathway Sources: Amigo / EGO
RNA expression pattern
250px
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	6870	21338
Ensembl	ENSG00000169836	ENSMUSG00000028172
UniProt	P29371	Q6NXX1
RefSeq (mRNA)	NM_001059	NM_021382
RefSeq (protein)	NP_001050	NP_067357
Location (UCSC)	Chr 4: 104.73 - 104.86 Mb	Chr 3: 134.77 - 134.87 Mb
PubMed search	[1]	[2]

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.

Function

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 neurokinin 3, also referred to as neurokinin B.

Selective ligands

Several selective ligands are available for NK₃, with two compounds osanetant and talnetant currently in clinical trials for treatment of schizophrenia and other indications.

Agonists

• Senktide - 7-amino acid polypeptide, NK₃ selective, CAS# 106128-89-6

Antagonists

• Osanetant
• Talnetant
• SB-222,200 - potent and selective antagonist, K_i = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, CAS# 174635-69-9
• SB-218,795 - more selective than SB-222,200, K_i = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1

See also

• Tachykinin receptor

Further reading

• Khawaja AM, Rogers DF (1996). "Tachykinins: receptor to effector". Int. J. Biochem. Cell Biol. 28 (7): 721–38. doi:10.1016/1357-2725(96)00017-9. PMID 8925404. 
• Advenier C, Lagente V, Boichot E (1997). "The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough". Eur. Respir. J. 10 (8): 1892–906. doi:10.1183/09031936.97.10081892. PMID 9272936. CS1 maint: Multiple names: authors list (link)
• Buell G, Schulz MF, Arkinstall SJ; et al. (1992). "Molecular characterisation, expression and localisation of human neurokinin-3 receptor". FEBS Lett. 299 (1): 90–5. doi:10.1016/0014-5793(92)80107-R. PMID 1312036. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Takahashi K, Tanaka A, Hara M, Nakanishi S (1992). "The primary structure and gene organization of human substance P and neuromedin K receptors". Eur. J. Biochem. 204 (3): 1025–33. doi:10.1111/j.1432-1033.1992.tb16724.x. PMID 1312928. CS1 maint: Multiple names: authors list (link)
• Xie GX, Miyajima A, Goldstein A (1992). "Expression cloning of cDNA encoding a seven-helix receptor from human placenta with affinity for opioid ligands". Proc. Natl. Acad. Sci. U.S.A. 89 (9): 4124–8. doi:10.1073/pnas.89.9.4124. PMC 525645 Freely accessible. PMID 1315051. CS1 maint: Multiple names: authors list (link)
• Huang RR, Cheung AH, Mazina KE; et al. (1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochem. Biophys. Res. Commun. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Dion S, Corcos J, Carmel M; et al. (1988). "Substance P and neurokinins as stimulants of the human isolated urinary bladder". Neuropeptides. 11 (2): 83–7. doi:10.1016/0143-4179(88)90015-7. PMID 2452993. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Krause JE, Staveteig PT, Mentzer JN; et al. (1997). "Functional expression of a novel human neurokinin-3 receptor homolog that binds [3H]senktide and [125I-MePhe7]neurokinin B, and is responsive to tachykinin peptide agonists". Proc. Natl. Acad. Sci. U.S.A. 94 (1): 310–5. doi:10.1073/pnas.94.1.310. PMC 19326 Freely accessible. PMID 8990205. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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. CS1 maint: Multiple names: authors list (link)
• Page NM, Woods RJ, Gardiner SM; et al. (2000). "Excessive placental secretion of neurokinin B during the third trimester causes pre-eclampsia". Nature. 405 (6788): 797–800. doi:10.1038/35015579. PMID 10866201. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 11786503. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• 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 Freely accessible. PMID 12477932. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Graham GJ, Stevens JM, Page NM; et al. (2005). "Tachykinins regulate the function of platelets". Blood. 104 (4): 1058–65. doi:10.1182/blood-2003-11-3979. PMID 15130944. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Gerhard DS, Wagner L, Feingold EA; et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928 Freely accessible. PMID 15489334. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Page NM, Dakour J, Morrish DW (2006). "Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia". Mol. Hum. Reprod. 12 (7): 427–33. doi:10.1093/molehr/gal025. PMID 16709596. CS1 maint: Multiple names: authors list (link)

External links

• "Tachykinin Receptors: NK₃". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

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