AT-121

AT-121 is a dual µ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPgammaS binding to cell membranes expressing µ-opioid or nociceptin receptors (EC50s = 19.6 and 34.7 nM, respectively). AT-121 (0.003-0.03 mg/kg) decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner. It lacks reinforcing effects, a marker of abuse potential, and reduces oxycodone, but not food pellet, reinforcement in a drug self-administration assay in rhesus monkeys when administered at doses ranging from 0.3 to 10 µg/kg per injection. AT-121 (0.01 or 0.03 mg/kg) does not induce hyperalgesia, a marker of tolerance development, in rhesus monkeys.Formal Name: N-[2-[1,2-dihydro-1'-[cis-4-(1-methylethyl)cyclohexyl]-3-oxospiro[isoquinoline-4(3H),4'-piperidin]-2-yl]ethyl]-sulfamide. CAS Number: 2099681-31-7. Molecular Formula: C24H38N4O3S. Formula Weight: 462.6. Purity: >95%. Formulation: (Request formulation change), A solution in chloroform. Solubility: Chloroform: 10 mg/ml, DMF: miscible, DMSO: miscible, Ethanol: miscible, Ethanol:PBS (pH 7.2) (1:20): 50µg/ml. SMILES: CC(C)[C@@H]1CC[C@H](N2CCC3(C(N(CCNS(N)(=O)=O)CC4=C3C=CC=C4)=O)CC2)CC1. InChi Code: InChI=1S/C24H38N4O3S/c1-18(2)19-7-9-21(10-8-19)27-14-11-24(12-15-27)22-6-4-3-5-20(22)17-28(23(24)29)16-13-26-32(25,30)31/h3-6,18-19,21,26H,7-17H2,1-2H3,(H2,25,30,31)/t19-,21+. InChi Key: LIZMNXKYQXVRSS-TYKWCNGQSA-N.