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Tachykinin receptor 3

Template:Infobox3cols/rowTemplate:Infobox3cols/rowTemplate:Infobox3cols/rowTemplate:Infobox3cols/row
Identifiers
SymbolsTACR3 ; HH11; NK-3R; NK3R; NKR; TAC3RL
External IDsOMIM162332 MGI892968 HomoloGene824 IUPHAR: 362 ChEMBL: 4429 GeneCards: TACR3 Gene
RNA expression pattern
File:PBB GE TACR3 208183 at tn.png
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez687021338
EnsemblENSG00000169836ENSMUSG00000028172
UniProtP29371P47937
RefSeq (mRNA)NM_001059NM_021382
RefSeq (protein)NP_001050NP_067357
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.[1][2]

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.[2]

Selective ligands

Several selective ligands are available for NK3. Two compounds osanetant and talnetant are being developed for treatment of various indications.[3]

Agonists

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

Antagonists

  • Osanetant
  • Talnetant
  • SB-222,200 - potent and selective antagonist, Ki = 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, Ki = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1

See also

References

  1. ^ Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (April 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochem. Biophys. Res. Commun. 184 (2): 966–72. PMID 1374246. doi:10.1016/0006-291X(92)90685-E. 
  2. ^ a b "Entrez Gene: TACR3 tachykinin receptor 3". 
  3. ^ Quartara L, Altamura M (August 2006). "Tachykinin receptors antagonists: from research to clinic". Curr Drug Targets 7 (8): 975–92. PMID 16918326. doi:10.2174/138945006778019381. 

Further reading

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External links

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

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