Tachykinin receptor 3

Tachykinin receptor 3
Identifiers
Symbols	TACR3; HH11; NK-3R; NK3R; NKR; TAC3RL
External IDs	OMIM: 162332 MGI: 892968 HomoloGene: 824 IUPHAR: NK3 ChEMBL: 4429 GeneCards: TACR3 Gene
Gene Ontology Molecular function • tachykinin receptor activity Cellular component • nucleus • plasma membrane • integral to plasma membrane Biological process • tachykinin receptor signaling pathway • aging • positive regulation of heart rate • response to estradiol stimulus • regulation of dopamine metabolic process • response to cocaine • hyperosmotic salinity response • response to morphine • positive regulation of blood pressure • regulation of feeding behavior • positive regulation of uterine smooth muscle contraction Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	6870	21338
Ensembl	ENSG00000169836	ENSMUSG00000028172
UniProt	P29371	P47937
RefSeq (mRNA)	NM_001059.2	NM_021382.6
RefSeq (protein)	NP_001050.1	NP_067357.1
Location (UCSC)	Chr 4: 104.51 – 104.64 Mb	Chr 3: 134.83 – 134.93 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. Two compounds osanetant and talnetant are being developed for treatment of various 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. 
• 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. 
• 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. 
• 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. PMID 1315051. //www.ncbi.nlm.nih.gov/pmc/articles/PMC525645/. 
• 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. 
• 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. 
• Krause JE, Staveteig PT, Mentzer JN et al. (1997). "Functional expression of a novel human neurokinin-3 receptor homolog that binds 3Hsenktide and 125I-MePhe7neurokinin 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. PMID 8990205. //www.ncbi.nlm.nih.gov/pmc/articles/PMC19326/. 
• 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. 
• 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. 
• 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. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1573107/. 
• 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. //www.ncbi.nlm.nih.gov/pmc/articles/PMC139241/. 
• 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. 
• 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. PMID 15489334. //www.ncbi.nlm.nih.gov/pmc/articles/PMC528928/. 
• 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. 

External links

• "Tachykinin Receptors: NK₃". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3031. 

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