Frances H, Simon P
Neuropharmacology. 1985 Jul;24(7):659-63. doi: 10.1016/0028-3908(85)90109-1.
Imipramine hydrochloride shows effects in a battery of tests used for the screening of antidepressant drugs. The central origin of these pharmacological effects of imipramine has not been clearly established. Imipramine methiodide is a quaternary derivative of imipramine which does not cross the blood-brain barrier easily. The effects of the two forms of imipramine have been compared: on an effect known to have a central origin; on two effects known to have a peripheral origin; on a battery of tests used for the screening of antidepressant drugs. It has been demonstrated that imipramine methiodide is as active as imipramine hydrochloride on two effects of peripheral origin, less active than imipramine hydrochloride on an effect considered to have a central origin and less active than imipramine hydrochloride or inactive on the tests which are used for the screening of antidepressant drugs. Consequently, the tests used for the screening of antidepressant drugs represent, primarily or exclusively, effects of central origin.
盐酸丙咪嗪在一系列用于筛选抗抑郁药物的测试中显示出效果。丙咪嗪这些药理作用的中枢起源尚未明确确定。甲碘丙咪嗪是丙咪嗪的季铵衍生物，不易穿过血脑屏障。已比较了两种形式丙咪嗪的作用：对已知有中枢起源的一种作用；对已知有外周起源的两种作用；对一系列用于筛选抗抑郁药物的测试。结果表明，甲碘丙咪嗪在外周起源的两种作用上与盐酸丙咪嗪活性相当，在一种被认为有中枢起源的作用上比盐酸丙咪嗪活性低，在用于筛选抗抑郁药物的测试中比盐酸丙咪嗪活性低或无活性。因此，用于筛选抗抑郁药物的测试主要或完全代表中枢起源的作用。
