Osanetant (hydrate)

Osanetant is a neurokinin-3 (NK3) receptor antagonist (Ki = 0.21 nM in CHO cells expressing the human receptor). It is selective for NK3 over NK1 and NK2 receptors (Kis = >100 and 0.02 µM, respectively). Osanetant inhibits contractions and acetylcholine release induced by neurokinin B (Cay-24542) in isolated guinea pig ileal strips in a concentration-dependent manner. It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) neutrophil, eosinophil, and lymphocyte infiltration in an ovalbumin-sensitized mouse model of allergic asthma. Osanetant (5 and 10 mg/kg) increases the duration of social interaction, as well as reduces immobility time in the tonic immobility test, indicating anxiolytic-like and antidepressant-like activities, respectively, in gerbils.Formal Name: N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-methyl-acetamide, monohydrate. Synonyms: SR 142801. Molecular Formula: C35H41Cl2N3O2 . H2O. Formula Weight: 624.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 15 mg/ml. SMILES: O=C(C1=CC=CC=C1)N(CCC2)C[C@]2(C3=CC(Cl)=C(C=C3)Cl)CCCN4CCC(C5=CC=CC=C5)(N(C)C(C)=O)CC4.O. InChi Code: InChI=1S/C35H41Cl2N3O2.H2O/c1-27(41)38(2)35(29-13-7-4-8-14-29)19-23-39(24-20-35)21-9-17-34(30-15-16-31(36)32(37)25-30)18-10-22-40(26-34)33(42)28-11-5-3-6-12-28,/h3-8,11-16,25H,9-10,17-24,26H2,1-2H3,1H2/t34-,/m0./s1. InChi Key: TZLATIVNEFZPKP-GXUZKUJRSA-N.