当前位置: X-MOL 学术J. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and central dopaminergic effects of N-(4,6-dimethyl-2-pyridinyl)benzamides.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 1985 May
Bouhayat, S, Piessard, S, Le Baut, G, Sparfel, L, Petit, J Y, Piriou, F, Welin, L

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.

中文翻译:

N-(4,6-二甲基-2-吡啶基)苯甲酰胺的合成及其中心多巴胺能作用。

合成了N-(4,6-二甲基-2-吡啶基)苯甲酰胺1-24和相应的三级衍生物29-33,并通过测试它们对幼稚和再固定化小鼠运动的影响来研究其对多巴胺的抑制作用。与原丙酰胺不同,它们没有显示出任何抗多巴胺能的特性,但是一些次生衍生物反而显示了突触后多巴胺能激动作用。随后研究了后一种化合物对利血平诱导的运动障碍的阿扑吗啡逆转以及对大鼠脑HVA水平的影响。化合物11在6-羟基多巴胺损伤小鼠中引起的相反盘旋表明涉及直接机制。
更新日期:2017-01-31
down
wechat
bug