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 NK<sub>3</sub>. NK<sub>3</sub> receptor antagonists are being investigated as treatments for various indications.
Agonists
- Neurokinin B â endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK<sub>3</sub>
- Senktide â 7-amino acid polypeptide, NK<sub>3</sub> 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 â potent and selective antagonist, K<sub>i</sub> = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, CAS# 174635-69-9
- SB-218,795 â more selective than SB-222,200, K<sub>i</sub> = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1
See also
References
Further reading
External links