Tachykinin receptor 3

TACR3
Identifiers
Aliases	TACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3
External IDs	MGI: 892968 HomoloGene: 824 GeneCards: TACR3
Targeted by Drug
eledoisin, Kassinin, substance p, osanetant, saredutant[1]
Gene ontology Molecular function • tachykinin receptor activity • G-protein coupled receptor activity • signal transducer activity • protein binding Cellular component • cytoplasm • integral component of membrane • membrane • plasma membrane • integral component of plasma membrane • dendrite membrane • neuronal cell body membrane • nucleus Biological process • G-protein coupled receptor signaling pathway • response to estradiol • aging • hyperosmotic salinity response • regulation of feeding behavior • regulation of dopamine metabolic process • positive regulation of heart rate • response to morphine • positive regulation of blood pressure • signal transduction • positive regulation of uterine smooth muscle contraction • response to cocaine • tachykinin receptor signaling pathway 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	NM_021382
RefSeq (protein)	NP_001050.1	NP_067357.1
Location (UCSC)	Chr 4: 103.59 – 103.72 Mb	Chr 3: 134.83 – 134.93 Mb
PubMed search	[2]	[3]
Wikidata

View/Edit Human

View/Edit Mouse

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.^[4][5]

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.^[5]

Selective ligands

Several selective ligands are available for NK₃. Two compounds osanetant and talnetant are being developed for treatment of various indications.^[6]

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

References

1. "Drugs that physically interact with Neuromedin-K receptor view/edit references on wikidata".
2. "Human PubMed Reference:".
3. "Mouse PubMed Reference:".
4. Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (Apr 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochemical and Biophysical Research Communications. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.
5. "Entrez Gene: TACR3 tachykinin receptor 3".
6. Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research to clinic". Current Drug Targets. 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326.

Further reading

• Khawaja AM, Rogers DF (Jul 1996). "Tachykinins: receptor to effector". The International Journal of Biochemistry & Cell Biology. 28 (7): 721–38. doi:10.1016/1357-2725(96)00017-9. PMID 8925404.
• Advenier C, Lagente V, Boichot E (Aug 1997). "The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough". The European Respiratory Journal. 10 (8): 1892–906. doi:10.1183/09031936.97.10081892. PMID 9272936.
• Buell G, Schulz MF, Arkinstall SJ, Maury K, Missotten M, Adami N, Talabot F, Kawashima E (Mar 1992). "Molecular characterisation, expression and localisation of human neurokinin-3 receptor". FEBS Letters. 299 (1): 90–5. doi:10.1016/0014-5793(92)80107-R. PMID 1312036.
• Takahashi K, Tanaka A, Hara M, Nakanishi S (Mar 1992). "The primary structure and gene organization of human substance P and neuromedin K receptors". European Journal of Biochemistry / FEBS. 204 (3): 1025–33. doi:10.1111/j.1432-1033.1992.tb16724.x. PMID 1312928.
• Xie GX, Miyajima A, Goldstein A (May 1992). "Expression cloning of cDNA encoding a seven-helix receptor from human placenta with affinity for opioid ligands". Proceedings of the National Academy of Sciences of the United States of America. 89 (9): 4124–8. doi:10.1073/pnas.89.9.4124. PMC 525645. PMID 1315051.
• Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (Apr 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochemical and Biophysical Research Communications. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.
• Dion S, Corcos J, Carmel M, Drapeau G, Regoli D (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, Schmidt SK, Tucker JB, Brodbeck RM, Bu JY, Karpitskiy VV (Jan 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". Proceedings of the National Academy of Sciences of the United States of America. 94 (1): 310–5. doi:10.1073/pnas.94.1.310. PMC 19326. PMID 8990205.
• Brunelleschi S, Bordin G, Colangelo D, Viano I (Jun 1998). "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, Lomthaisong K, Gladwell RT, Butlin DJ, Manyonda IT, Lowry PJ (Jun 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, Cucchi P, Lecci A, Meini S, Patacchini R, Quartara L, Ricci R, Tramontana M, Giuliani S, Maggi CA (Jan 2002). "Pharmacological profile of the novel mammalian tachykinin, hemokinin 1". British Journal of Pharmacology. 135 (1): 266–74. doi:10.1038/sj.bjp.0704443. PMC 1573107. PMID 11786503.
• Graham GJ, Stevens JM, Page NM, Grant AD, Brain SD, Lowry PJ, Gibbins JM (Aug 2004). "Tachykinins regulate the function of platelets". Blood. 104 (4): 1058–65. doi:10.1182/blood-2003-11-3979. PMID 15130944.
• Page NM, Dakour J, Morrish DW (Jul 2006). "Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia". Molecular Human Reproduction. 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.

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