enadoline

Enadoline is a highly selective and potent κ-opioid receptor agonist developed as an analgesic. It is an arylacetamide-derived small molecule with strong affinity for the kappa-opioid receptor (KOR), showing minimal activity at mu-opioid receptors. In preclinical and clinical studies, enadoline demonstrated significant antinociceptive (pain-blocking) effects, being much more potent than morphine in animal models. However, its development was discontinued due to dose-limiting neuropsychiatric adverse events such as dysphoria, visual distortions, depersonalization, sedation, confusion, and other psychotomimetic effects. Unlike typical mu-opioid agonists like morphine or hydromorphone, enadoline did not cause respiratory depression but produced dissociative symptoms reminiscent of salvinorin A. There was some consideration for its use in comatose head injury or stroke patients where neuropsychiatric side effects would be less relevant[1][3][4][5][7].

Other names

EnadolinaCam 569Cam569Cam-569