PD-117302

PD-117302 is a synthetic small molecule that acts as a highly selective agonist of the κ-opioid receptor. It was originally developed by Parke-Davis as part of a series of arylacetamide kappa opioids for analgesic and neuroprotective purposes. The compound demonstrates approximately 9000-fold selectivity for the κ-opioid receptor over mu or delta opioid receptors, with negligible affinity for non-opioid sites such as PCP or sigma receptors. In preclinical studies, PD-117302 has shown potent analgesic effects in animal models by raising the nociceptive threshold to mechanical and chemical stimuli but not thermal stimuli. Additionally, it exhibits antiarrhythmic properties through direct blockade of multiple cardiac ion channels—reducing peak sodium current and blocking outward potassium currents—which results in ECG changes and reduced arrhythmia incidence in rats. Despite its promising pharmacological profile, there is no evidence that it advanced to clinical development or approval[1][2][6][8][9].

Other names

(±)-trans-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzo[b]thiophene-4-acetamide