Aticaprant

Aticaprant is a kappa-opioid receptor (KOR) antagonist (Ki = 0.807 nM). It is selective for KOR over the µ- and delta-opioid receptors (Kis = 24 and 155 nM, respectively). Aticaprant reverses U-69593-induced decreases in nocifensive behavior in the formalin test in rats (ED50 = 0.4 mg/kg). It also reverses U-69593-induced disruptions in prepulse inhibition in rats in a dose-dependent manner. Aticaprant (10 mg/kg) reduces immobility time in the forced swim test in mice. It reduces alcohol self-administration and the progressive ratio breakpoint in rats when administered at a dose of 10 mg/kg.Formal Name: 4-[4-[[(2S)-2-(3,5-dimethylphenyl)-1-pyrrolidinyl]methyl]phenoxy]-3-fluoro-benzamide. CAS Number: 1174130-61-0. Synonyms: CERC-501, JNJ-67953964, LY2456302. Molecular Formula: C26H27FN2O2. Formula Weight: 418.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, Ethanol: 3 mg/ml. SMILES: NC(C1=CC(F)=C(C=C1)OC(C=C2)=CC=C2CN3CCC[C@H]3C4=CC(C)=CC(C)=C4)=O. InChi Code: InChI=1S/C26H27FN2O2/c1-17-12-18(2)14-21(13-17)24-4-3-11-29(24)16-19-5-8-22(9-6-19)31-25-10-7-20(26(28)30)15-23(25)27/h5-10,12-15,24H,3-4,11,16H2,1-2H3,(H2,28,30)/t24-/m0/s1. InChi Key: ZHPMYDSXGRRERG-DEOSSOPVSA-N.