Tachykinin receptor 3
Protein-coding gene in the species Homo sapiens
From Wikipedia, the free encyclopedia
Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.[5][6]
External IDsOMIM: 162332; MGI: 892968; HomoloGene: 824; GeneCards: TACR3; OMA:TACR3 - orthologs
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.[6]
Selective ligands
A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications.[7]
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, 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
