Nepinalone is a new alchilaminate derivative of β-tetralone, which possess a non-opioid antitussive activity. Nepinalone racemus exerted a significant antitussive activity and both L- and D-isomers confirmed to possess a significant dose-correlated antitussive effect with better trend of activity for D-isomer, but not statistically significant. It was predicted to act via sigma receptors. Occasionally, episodes of gastric intolerance have been reported and rapidly receded when treatment was stopped. The use of doses higher than those recommended could cause drowsiness.