Synthesis and Central Dopaminergic Effects of N-(4,6-Dimethyl-2-pyridinyl)benzamides

Abstract
N-(4,6-Dimethyl-2-pyridinyl)benzamides and the corresponding tertiary derivatives were synthesized and studied for possible dopamine-inhibitory properties by testing their effect on motility of naive and reserpinized mice. Unlike the orthopramides, they failed to show any antidopaminergic properties, but some of the secondary derivatives showed instead effects of postsynaptic dopaminergic agonism. The latter compounds were subsequently studied for their effects on apomorphine reversal of reserpine-induced alkinesia and on cerebral HVA [homovanillic acid] levels in rats. Contraversive circling induced by 1 compound in 6-hydroxydopamine-lesioned mice suggests that a direct mechanism was involved.