Tachykinin receptor 3

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Tachykinin receptor 3
Identifiers
Symbols TACR3 ; HH11; NK-3R; NK3R; NKR; TAC3RL
External IDs OMIM162332 MGI892968 HomoloGene824 IUPHAR: NK3 ChEMBL: 4429 GeneCards: TACR3 Gene
RNA expression pattern
PBB GE TACR3 208183 at tn.png
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 NP_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[edit]

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[edit]

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

Agonists[edit]

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

Antagonists[edit]

  • 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[edit]

References[edit]

  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. doi:10.1016/0006-291X(92)90685-E. PMID 1374246. 
  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. doi:10.2174/138945006778019381. PMID 16918326. 

Further reading[edit]

External links[edit]

  • "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.