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2-(亚甲基氨氧基)甲基吗啉衍生物。合成与抗抑郁活性。

2-(Methyleneaminoxy)methylmorpholine derivatives. Synthesis and antidepressant activity.

作者信息

Balsamo A, Lapucci A, Macchia M, Martinelli A, Nencetti S, Rossello A, Cristina T

机构信息

Istituto di Chimica Farmaceutica e Tossicologica, Facoltà di Farmacia, Pisa, Italy.

出版信息

Farmaco. 1994 Feb;49(2):77-82.

PMID:8003184
Abstract

The 3-(methyleneaminoxy)methylmorpholines 2 were synthesized as analogues of viloxazine 1, an antidepressant drug, in which the aryloxymethyl group is substituted by a (methyleneaminoxy)methyl moiety (MAOMM). Compounds 2 were tested as potential antidepressant agents by using the test of antagonism to reserpine-induced hypothermy in mice. In addition, their anticholinergic and antihistaminic activity on isolated preparations and their ability to antagonize the toxicity induced by adrenaline in mice were evaluated. "In vivo" and "in vitro" tests showed that some compounds of type 2 possess a pharmacological profile similar to that of viloxazine 1.

摘要

合成了3-(亚甲基氨氧基)甲基吗啉2作为抗抑郁药维洛沙嗪1的类似物,其中芳氧基甲基被(亚甲基氨氧基)甲基部分(MAOMM)取代。通过对小鼠利血平诱导的体温过低进行拮抗试验,将化合物2作为潜在的抗抑郁药进行测试。此外,还评估了它们对离体标本的抗胆碱能和抗组胺活性以及拮抗小鼠肾上腺素诱导毒性的能力。“体内”和“体外”试验表明,一些2型化合物具有与维洛沙嗪1相似的药理特性。

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