GANGLIONIC BLOCKING ACTION OF SOME METHYLPIPERIDINES

¹ Department of Pharmacology, School of Medicine, Montevideo, Uruguay

We have studied several methylpiperidines, as their hydrochlorides or as quaternary methosalts. 2-Methyl-, 1,2-dimethyl-, 1,4-dimethylpiperidines and the methiodides of the last two are ganglionic blocking drugs, although the doses required for this action are relatively large. Much more potent are 2,6-dimethylpiperidine, 1,2,6-trimethylpiperidine and its methobromide. The most potent compound used is the secondary 2,2,6,6-tetramethylpiperidine. The ganglionic block produced by secondary and tertiary amines is markedly long lasting. The quaternary compounds are more active in equimolar doses, their effects being of shorter duration. We have demonstrated that the presence of at least three methyl groups in positions 2 and 6 of the substituted piperidine ring is not absolutely necessary to confer ganglionic blocking properties upon the molecule, although it has been confirmed that increasing the number of methyl substituents at the 2- and 6-positions augments the ganglionic blocking action. Bis-1,2,6-trimethylpiperidine-p-xylilene dibromide has curarelike properties as well as gangliomc blocking actions. The ganglionic block produced by all of these derivatives was of the nondepolarizing type.