Local Anesthetic Activity of a Series of Phenyl Piperidine Derivatives. ∗

Abstract

Summary

A number of new phenylpiperi-dine derivatives (a-4-methyl-(III), β-4-me-thyl-(IV), 4-dimethyl-(V), 4-methylol-(VI), α-4-phenyl-(VII), β-4-phenyl-(VIII), α-4-carboxylic acid-(X), α-4-carbomethoxy-(XI), α-4-carbethoxy- (XII), 3-phenyl-piperidine) were found to produce anesthesia after intra-dermal injection in guinea-pigs which was more prolonged than that observed after procaine. All of the new compounds induced hyperemia followed in most cases by necrosis at the site of injection. After topical application 1.0% solutions of III, IV, V, VII or VIII produced corneal anesthesia in rabbits. In 1.0% solutions VI, X, XI or XII failed to exhibit topical activity in rabbits. Intra-peritoneally in mice the acute toxicity of the new derivatives was in the range of that of cocaine.