Tachykinin receptor 3

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

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

A number of selective ligands are available for NK₃. NK₃ receptor antagonists are being investigated as treatments for various indications.

Agonists

• Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK₃
• Senktide – 7-amino acid polypeptide, NK₃ selective, CAS# 106128-89-6

Antagonists

• Elinzanetant (BAY-3427080 GSK-1144814, NT-814)
• Fezolinetant (ESN-364)
• Osanetant (SR-142,801)
• Pavinetant (MLE-4901, AZD-4901, AZD-2624)
• Talnetant (SB-223,412)
• SB-222,200 – potent and selective antagonist, K_i = 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, K_i = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1

See also

• Tachykinin receptor

External links

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