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
- Fezolinetant
- Osanetant
- Pavinetant
- Talnetant
- SB-222,200 – potent and selective antagonist, Ki = 4.4 nM, 3-Methyl-2-phenyl-N--4-quinolinecarboxamide, CAS# 174635-69-9
- SB-218,795 – more selective than SB-222,200, Ki = 13 nM, --methyl ester benzeneacetic acid, CAS# 174635-53-1