Young R, Darmani N A, Elder E L, Dumas D, Glennon R A
Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia/Virginia, Commonwealth University, Richmond 23298-0540, USA.
Pharmacol Biochem Behav. 1997 Feb;56(2):311-6. doi: 10.1016/s0091-3057(96)00329-2.
Clobenzorex, an optically active N-substituted derivative of (+)amphetamine, has been identified on the illicit market. Because so little is known regarding the pharmacology or abuse potential of this agent, it was examined in tests of stimulus generalization in rats trained to discriminate 1 mg/kg of (+)amphetamine from vehicle to determine if it would produce amphetamine-appropriate responding. Clobenzorex (ED50 = 6.6 mg/kg) substituted for (+)amphetamine (ED50 = 0.3 mg/kg) but was approximately twenty times less potent than the training drug. Clobenzorex was also compared with (+)amphetamine and cocaine for its ability to induce locomotor stimulation and rearing frequency in mice. Clobenzorex was active in both assays but was less potent than either (+)amphetamine or cocaine. It is concluded that, although weaker than (+)amphetamine, clobenzorex constitutes an agent with amphetamine-like central stimulant behavioral properties.
氯苄雷司，一种（+）苯丙胺的旋光性N-取代衍生物，已在非法市场上被发现。由于对该药物的药理学或滥用潜力了解甚少，因此在训练大鼠区分1mg/kg（+）苯丙胺和赋形剂的刺激泛化试验中对其进行了研究，以确定它是否会产生与苯丙胺相符的反应。氯苄雷司（半数有效量=6.6mg/kg）可替代（+）苯丙胺（半数有效量=0.3mg/kg），但其效力约为训练药物的二十分之一。还将氯苄雷司与（+）苯丙胺和可卡因在诱导小鼠运动兴奋和竖毛频率方面的能力进行了比较。氯苄雷司在两种试验中均有活性，但效力低于（+）苯丙胺或可卡因。得出的结论是，尽管氯苄雷司比（+）苯丙胺弱，但它是一种具有类似苯丙胺中枢兴奋行为特性的药物。
