An NK3 receptor antagonist (Ki = 0.013 µM), selective for NK3 over NK1 and NK2 receptors (Kis = >100 and 1.221 µM, respectively), inhibits senktide-induced contractions in isolated rabbit iris sphincter muscle preparations (Kb = 43 nM), inhibits substance P-induced contraction of longitudinal and circular smooth...

Description: SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1. Target: Neurokinin receptor. Smiles: C(N[C@@H](C(OC)=O)C1=CC=CC=C1)(=O)C=2C3=C(N=C(C2)C4=CC=CC=C4)C=CC=C3. References: Medhurst AD, et, al. In vitro and...