Tachykinin receptor 3

Tachykinin receptor 3

Tachykinin receptor 3
Identifiers
TACR3 Gene
RNA expression pattern

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

Further reading

External links

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