Pravadoline

Pravadoline is a cannabimimetic aminoalkylindole agonist of the cannabinoid receptors and an inhibitor of Cox-1 and Cox-2, demonstrating powerful analgesic effects through the combination of these actions. Pravadoline was developed for Cox inhibition activity and was found to produce analgesic effects at concentrations much lower than needed for Cox inhibition, leading to the observation of Pravadoline-induced inhibition of neuronally mediated smooth muscle contractions distinct from the activity of opioid analgesics. The cannabimimetic activity of Pravadoline was identified in comparison with the binding of CP-55940, and derivatives of the aminoalkylindole have been subsequently explored towards generating specific cannabinoid receptor agonists.