Tachykinin receptor 3

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TACR3
Identifiers
Aliases TACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3
External IDs MGI: 892968 HomoloGene: 824 GeneCards: 6870
RNA expression pattern
PBB GE TACR3 208183 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
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 [1] [2]
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.[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 (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. 
  2. ^ a b "Entrez Gene: TACR3 tachykinin receptor 3". 
  3. ^ 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[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.