[1][2] It is several hundred times selective for the ORL-1 receptor over other opioid receptors,[3][4] and its effects in animals include preventing the development of tolerance to morphine,[5] the prevention of hyperalgesia induced by intracerebroventricular administration of nociceptin (orphanin FQ),[6] as well as the stimulation of dopamine release in the striatum,[7] which increases the rewarding effects of cocaine,[8] but may have clinical application in the treatment of Parkinson's disease.

Reaction with boc anhydride followed by treatment with trifluoroacetic acid gives CID:16726358 (4).

Reaction with iodoethane in the presence of base alkylates the urea nitrogen giving CID:16726359 (5).

Reduction of the enamine by treatment with magnesium metal in methanol solvent occurs to give predominantly the trans isomer, CID:16726360 (6).

Lastly, reduction of the ester with lithium aluminium hydride completed the synthesis of J-113397 (10).