Bouhayat S, Piessard S, Le Baut G, Sparfel L, Petit J Y, Piriou F, Welin L
J Med Chem. 1985 May;28(5):555-9. doi: 10.1021/jm50001a004.
N-(4,6-Dimethyl-2-pyridinyl)benzamides 1-24 and the corresponding tertiary derivatives 29-33 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 akinesia and on cerebral HVA levels in rats. Contraversive circling induced by compound 11 in 6-hydroxydopamine-lesioned mice suggests that a direct mechanism was involved.
合成了N-(4,6-二甲基-2-吡啶基)苯甲酰胺1-24以及相应的叔衍生物29-33，并通过测试它们对未用药和利血平化小鼠运动能力的影响，研究其可能的多巴胺抑制特性。与邻苯甲酰胺不同，它们未表现出任何抗多巴胺能特性，但一些仲衍生物反而表现出突触后多巴胺能激动作用。随后研究了后一类化合物对利血平诱导的运动不能的阿扑吗啡逆转作用以及对大鼠脑内高香草酸水平的影响。化合物11在6-羟基多巴胺损伤小鼠中诱导的反向旋转表明涉及直接机制。
