Drug protein interaction: inhibition of glutamate dehydrogenase by psycoactive butyrophenones.

8 psychoactive butyrophenones were assayed as inhibitors of bovine and tuna glutamate dehydrogenase (EC 1.4.1.2-4). Kinetic experiments indicated that the inhibitory action of butyrophenones is consequent to an increase of the inhibitory action of butyrophenones is consequent to an increase of the inhibition produced by the substrate. The inhibition constants of the various drugs were calculated and compared with their known pharmacological potencies as neuroleptics. A strict correlation between the inhibition of the enzyme and the in vivo properties was apparent since the drugs most active as inhibitors possess higher pharmacological activity.