spiradoline

Spiradoline is a synthetic small molecule that acts as a highly selective kappa-opioid receptor agonist. It was developed primarily for its analgesic (pain-relieving), diuretic (increasing urine output), antitussive (cough-suppressing), antiarrhythmic, and neuroprotective properties. Spiradoline exhibits high selectivity for the kappa-opioid receptor with much lower affinity for mu and delta opioid receptors. In preclinical studies and early clinical trials, it demonstrated potent analgesic and diuretic effects but also produced significant side effects in humans such as sedation, dysphoria (unease or dissatisfaction), hallucinations, and social avoidance behaviors. These adverse effects limited its clinical development despite promising pharmacological activity. Spiradoline also blocks sodium channels and potassium channels at higher concentrations in cardiac tissue—contributing to its antiarrhythmic profile[1][4][5][6].

Other names

spiradolineU-62066U62066U 62066U 62066EU62066EU-62066EPF-00345768PF00345768PF 00345768