HYPNOTIC ACTION OF CERTAIN TERTIARY BUTYL ALIPHATIC AMIDES

¹ From the Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee

The compounds listed in table 1 may be roughly grouped as follows:

1. Those which are ineffective in doses larger than 1 gram per kilogram.

2. Those which are effective as hypnotics in doses as large as 1 gram per kilogram.

3. Those which show convulsant activity.

4. Those which are lethal in sub-effective or minimum effective doses.

It is noted that the amides having the most marked hypnotic

[See table in the PDF file]

activity have in common an alpha-substituted bromine atom and N-substituted alkyl groups. Of these the most active was -bromo-tertiary-butyl-acetyl-dimethyl-amide with a therapeutic index of 2. In contrast to the action in the rabbit, this compound produced violent convulsions in the rat. Those compounds producing

[See table in the PDF file]

convulsions in the rabbit lacked the -bromine atom, but all possessed N-substituted alkyl groups. Although the number of tests with each compound have been relatively few, there is no evidence that any amide in the above series equals neuronal in hypnotic effectiveness.