Schechter M D, McBurney D
Department of Pharmacology, Northeastern Ohio Universities, College of Medicine, Rootstown 44272, USA.
Life Sci. 1996;59(20):PL303-8. doi: 10.1016/s0024-3205(96)00513-9.
Drug discrimination studies were conducted in six male Sprague-Dawley rats trained to discriminate the interoceptive cues produced by 10 mg/kg cocaine in an effort to investigate if there is stimulus generalization to phentermine or phentermine + fenfluramine. Once having reached criterion performance, these rats were tested with lower doses of cocaine and generated a typical dose-response curve allowing for calculation of an ED50 value: 2.798 mg/kg. Testing of phentermine in doses of 1.25-5.0 mg/kg indicated generalization with the highest dose producing 80% cocaine-appropriate responding and allowing for an ED50 value of 2.356 mg/kg. When the phentermine doses were tested in combination 2.0 mg/kg fenfluramine, however, there was an increase in the discriminability of the highest phentermine dose and a slight decrease in the ED50 value of the combination. Thus, administration of phentermine + fenfluramine, having both dopamine-releasing and serotonin-releasing properties, respectively, may mimic the neurochemical activity by which cocaine acts in the central nervous system and may possibly allow for cocaine-like effects as these two drugs see increased use in obesity control.
在六只雄性斯普拉格-道利大鼠身上进行了药物辨别研究,这些大鼠经过训练以辨别10毫克/千克可卡因产生的内感受性线索,目的是研究是否存在对苯丁胺或苯丁胺+芬氟拉明的刺激泛化现象。一旦达到标准表现,这些大鼠就用较低剂量的可卡因进行测试,并生成了一条典型的剂量-反应曲线,从而可以计算出半数有效剂量(ED50)值:2.798毫克/千克。对1.25 - 5.0毫克/千克剂量的苯丁胺进行测试表明存在泛化现象,最高剂量产生了80%与可卡因相符的反应,其ED50值为2.356毫克/千克。然而,当将苯丁胺剂量与2.0毫克/千克芬氟拉明联合测试时,最高苯丁胺剂量的辨别能力有所增加,联合用药的ED50值略有下降。因此,分别具有释放多巴胺和释放血清素特性的苯丁胺+芬氟拉明的给药,可能模仿了可卡因在中枢神经系统中起作用的神经化学活性,并且由于这两种药物在肥胖控制中的使用增加,可能会产生类似可卡因的效果。