论文部分内容阅读
本品是一种抗抑郁药和5-HT摄取抑制剂。合成在回流THF中,(±)-2-(3,4-二氯苄基)氨基丙酸(Ⅰ)用BH_3·S(CH_3)_2还原反应得(±)-2-氨基-3-(3,4-二氯苯基)-2-甲基丙醇(Ⅱ),在回流甲酸中,Ⅱ与甲醛经甲基化即得本品。药理作用体外本品选择性阻滞5-HT摄取,与[~3H]-帕罗西丁(paroxetine)和[~3H]-丙咪嗪结合位置亲合性高,但不阻滞MAO-A或MAO-B,与毒蕈碱、组胺或脑其它受体亲合性很小。在小鼠绝望行为试验中,本品减少
This product is an antidepressant and 5-HT uptake inhibitors. Synthesis The (±) -2- (3,4-dichlorobenzyl) aminopropionic acid (Ⅰ) was reduced with BH_3 · S (CH_3) _2 in refluxing THF to give (±) 3,4-dichlorophenyl) -2-methyl propanol (Ⅱ), in refluxing formic acid, Ⅱ and formaldehyde methylation obtained the goods. Pharmacological Action This product selectively blocks 5-HT uptake in vitro and has high affinity with the [~ 3H] -paroxetine and [~ 3H] -promazine binding sites but does not block MAO-A Or MAO-B, with little affinity for muscarinic, histamine or other brain receptors. Destructive behavior in mice test, the goods decreased