Demerson C A, Santroch G, Humber L G
J Med Chem. 1975 Jun;18(6):577-80. doi: 10.1021/jm00240a010.
A series of 3,4-dihydro-1H-1,4-oxazino[4,3-a]indoles bearing basic side chains has been synthesized by a novel chemical process. These compounds have been screened for potential antidepressant activity. One of these derivatives, 3,4-dihydro-1,10-dimethyl-1-(3-methylaminopropyl)-1H-1,4-oxazino[4,3-a]indole (AY-23,673), was particularly potent in the prevention of reserpine ptosis test in mice, with an ED50 of 0.5 mg/kg ip.
通过一种新的化学方法合成了一系列带有碱性侧链的3,4-二氢-1H-1,4-恶嗪并[4,3-a]吲哚。已对这些化合物进行潜在抗抑郁活性筛选。其中一种衍生物，3,4-二氢-1,10-二甲基-1-(3-甲氨基丙基)-1H-1,4-恶嗪并[4,3-a]吲哚（AY-23,673），在预防小鼠利血平致眼睑下垂试验中特别有效，腹腔注射的半数有效剂量（ED50）为0.5毫克/千克。
