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Modulation of Pharmacological Profile of Diphenylethane (Lefetamine-type) Derivatives

Modulation of Pharmacological Profile of Diphenylethane (Lefetamine-type) Derivatives

  1. Anonymous
    Maria Carrara et al.

    Summary
    With the aim to split the pharmacological properties of lefetamine (CAS 14148-99-3), some structural
    modifications of this compound have been studied. The basic group of lefetamine has been shifted from
    the alkyl chain to the vicinal phenyl ring and the N-substitution has been changed. The dimethylaminomethyl derivatives and chiefly the o-morpholinomethyl exhibited a strong anti-visceral chemical antinociception activity stripped of thermal antinociception properties and physical dependence liability.
    Furthermore, through the introduction of a diethylaminomethyl group in the lefetamine structure some derivatives were selected exhibiting besided a significant increase in the anti-visceral chemical antinociception activity, remarkable local anesthetic properties.