MODULATION OF PHARMACOLOGICAL PROFILE OF DIPHENYLETHANE (LEFETAMINE-TYPE) DERIVATIVES

With the aim to split the pharmacological properties of lefetamine (GA S 14148-99-3), some structural modifications of this compound have bee n studied. The basic group of lefetamine has been shifted from the alk yl chain to the vicinal phenyl ring and the N-substitution has been ch anged. The dimethylaminomethyl derivatives and chiefly the o-morpholin ometyhl exhibited a strong anti-visceral chemical antinociception acti vity stripped of thermal antinociception properties and physical depen dence liability. Furthermore, through the introduction of a diethylami nomethyl group in the lefetamine structure some derivatives were selec ted exhibiting besided a significant increase in the anti-visceral che mical antinociception activity, remarkable local anesthetic properties .