Tang A H, Cangelosi A A, Code R A, Franklin S R
Pharmacol Biochem Behav. 1984 Feb;20(2):209-13. doi: 10.1016/0091-3057(84)90244-2.
2-Methyl-3,3-diphenyl-3-propanolamine (2-MDP) produced effects in animals similar to those produced by the dissociative anesthetics such as phencyclidine (PCP). Specifically, it shared the discriminative stimulus properties of PCP in rats trained to discriminate PCP (1 mg/kg) from saline; at higher doses, it disrupted brightness discrimination and stimulated locomotor activities in rats trained to avoid shocks in an automated Y-maze; and it produced surgical anesthesia when injected IV to rhesus monkeys. These pharmacological activities were observed only with the levo-isomer of 2-MDP. The dextro-isomer was either inactive or produced opposite effects, depending on the tests. Among several related diphenylpropylamines, 2-MDP represents the optimal structure for potency of PCP-like effects since changes in the amino, 2-methyl and 3-hydroxy groups reduced the potencies of the PCP-like discriminative properties.
2-甲基-3,3-二苯基-3-丙醇胺(2-MDP)在动物身上产生的效应与诸如苯环己哌啶(PCP)等分离麻醉剂所产生的效应相似。具体而言,在经过训练以区分PCP(1毫克/千克)和生理盐水的大鼠中,它具有PCP的辨别刺激特性;在较高剂量下,它会干扰亮度辨别,并在经过训练以在自动Y迷宫中避免电击的大鼠中刺激运动活动;当静脉注射给恒河猴时,它会产生外科麻醉效果。这些药理活性仅在2-MDP的左旋异构体中观察到。右旋异构体要么无活性,要么根据测试产生相反的效果。在几种相关的二苯基丙胺中,2-MDP代表了产生PCP样效应效力的最佳结构,因为氨基、2-甲基和3-羟基的变化会降低PCP样辨别特性的效力。