Girish Mahajan (Editor)

Tachykinin receptor 3

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Species
  
Human

Entrez
  
6870

Human
  
Mouse

Ensembl
  
ENSG00000169836

Tachykinin receptor 3

Aliases
  
TACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3

External IDs
  
MGI: 892968 HomoloGene: 824 GeneCards: TACR3

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.

Contents

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, 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

    • References

    Tachykinin receptor 3 Wikipedia
    (Text) CC BY-SA