sch221510

**SCH221510** is a potent and selective small molecule agonist of the **nociceptin opioid receptor (NOP, also known as the N/OFQ receptor or OPRL1)**. It was developed as a tool compound to explore the pharmacology of NOP receptor agonism. SCH221510 exhibits anxiolytic-like and anti-addictive properties in preclinical models, showing robust anxiolytic efficacy in various animal anxiety paradigms at doses that do not impair locomotion or induce sedative effects. It also has potential analgesic effects with a different side effect profile compared to classical opioid agonists, lacking common opioid adverse effects such as constipation and respiratory depression. Further, SCH221510 can attenuate the reinforcing effects of mu opioid receptor agonists (like remifentanil and morphine), suggesting possible utility in the treatment of drug addiction and relapse. The compound is orally active and has been widely studied in vivo for anxiety and addiction models. Despite its promising preclinical profile, SCH221510 was not developed into clinical trials, possibly due to limitations in brain penetration or insufficient therapeutic window[1][2][3][4][5].

Other names

3-Endo-8-bis(2-methylphenyl)methyl-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol