J-113397

J-113397 is a potent, highly selective, nonpeptidyl antagonist of the nociceptin/orphanin FQ peptide receptor (NOP, also known as ORL-1). It is several hundred-fold more selective for the NOP receptor than for other classical opioid receptors (mu, delta, kappa), lacking significant actions on these other opioid subtypes at pharmacologically relevant concentrations[1][2][11][13]. In animal studies, J-113397 blocks the behavioral and biochemical effects induced by nociceptin/orphanin FQ, prevents tolerance development to morphine, modulates dopaminergic transmission in the striatum, attenuates hyperalgesia, and exhibits antidepressant-like and antiparkinsonian properties[1][2][4][7][10][12]. It is frequently used as a pharmacological tool in neuropharmacological research to dissect the role of NOP signaling in pain, mood disorders, and movement disorders, but it is not approved for medical use in humans.

Other names

1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one