GR159897

GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor. It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.Formal Name: 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole. CAS Number: 158848-32-9. Molecular Formula: C23H27FN2O2S. Formula Weight: 414.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 30 mg/ml. SMILES: O=[S@@](C1=CC=CC=C1)CC(OC)(CC2)CCN2CCC(C3=C4)=CNC3=CC=C4F. InChi Code: InChI=1S/C23H27FN2O2S/c1-28-23(17-29(27)20-5-3-2-4-6-20)10-13-26(14-11-23)12-9-18-16-25-22-8-7-19(24)15-21(18)22/h2-8,15-16,25H,9-14,17H2,1H3/t29-/m1/s1. InChi Key: BANYJBHWTOJQDU-GDLZYMKVSA-N.