Chronobiotic activity of N-[2-(2,7-dimethoxyfluoren-9-yl)ethyl]-propanamide. Synthesis and melatonergic pharmacology of fluoren-9-ylethyl amides

Compound 2b demonstrated full agonism at both human MT1 and MT2 receptors and demonstrated chronobiotic activity in both acute and chronic rat models, producing an acute phase advance of 32min at 1mg/kg and chronically entraining free-running rats with a mean effective dose of 0.23mg/kg. This compound was significantly less efficacious than melatonin in constricting human coronary artery.