Young R, Glennon R A
Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond 23298-0540, USA.
Psychopharmacology (Berl). 1998 Dec;140(3):250-6. doi: 10.1007/s002130050765.
Methcathinone ("CAT") is a CNS stimulant that is a very significant drug of abuse in the former Soviet Union. It has also appeared on the clandestine market in the United States and has been recently classified as a Schedule I substance. In the present study, S(-)-methcathinone [S(-)-CAT, 0.50 mg/kg, IP] was employed as the training drug in a two-lever drug discrimination task in rats. Once established, the S(-)-CAT stimulus was shown to have a rapid onset to action (within 5 min) and a duration of effect of approximately 60-90 min. In tests of stimulus generalization (substitution), the S(-)-CAT (ED50 = 0.11 mg/kg) stimulus generalized to S(+)-methamphetamine (ED5 = 0.17 mg/kg), S(-)-cathinone (ED50 = 0.19 mg/kg), S(+)-amphetamine (ED50 = 0.23 mg/kg), aminorex (ED50 = 0.27 mg/kg), (+/-)-CAT (ED50 = 0.25 mg/kg), (+/-)-cathinone (ED50 = 0.41 mg/kg), R(+)-CAT (ED50 = 0.43 mg/kg), cis-4-methylaminorex (ED50 = 0.49 mg/kg), methylphenidate (ED50 = 0.83 mg/kg), and cocaine (ED50= 1.47 mg/kg). S(-)-CAT-stimulus generalization did not occur to fenfluramine, a structurally related nonstimulant anorectic. Lastly, haloperidol (AD50 = 0.18 mg/kg), a dopamine receptor antagonist, potently antagonized the S(-)-CAT stimulus. It is concluded that S(-)-methcathinone is a very potent CNS stimulant, which appears to produce its stimulus effect, at least in part, via a dopaminergic mechanism.
甲卡西酮（“CAT”）是一种中枢神经系统兴奋剂，在前苏联是一种非常重要的滥用药物。它也出现在美国的地下市场，最近被列为一类管制物质。在本研究中，S(-)-甲卡西酮[S(-)-CAT，0.50mg/kg，腹腔注射]被用作大鼠双杠杆药物辨别任务中的训练药物。一旦建立，S(-)-CAT刺激显示起效迅速（5分钟内），作用持续时间约为60-90分钟。在刺激泛化（替代）测试中，S(-)-CAT（ED50 = 0.11mg/kg）刺激可泛化至S(+)-甲基苯丙胺（ED5 = 0.17mg/kg）、S(-)-去甲伪麻黄碱（ED50 = 0.19mg/kg）、S(+)-苯丙胺（ED50 = 0.23mg/kg）、阿米雷司（ED50 = 0.27mg/kg）、(+/-)-CAT（ED50 = 0.25mg/kg）、(+/-)-去甲伪麻黄碱（ED50 = 0.41mg/kg）、R(+)-CAT（ED50 = 0.43mg/kg）、顺式-4-甲基阿米雷司（ED50 = 0.49mg/kg）、哌甲酯（ED50 = 0.83mg/kg）和可卡因（ED50 = 1.47mg/kg）。S(-)-CAT刺激不会泛化至芬氟拉明，一种结构相关的非刺激性食欲抑制剂。最后，多巴胺受体拮抗剂氟哌啶醇（AD50 = 0.18mg/kg）可有效拮抗S(-)-CAT刺激。结论是S(-)-甲卡西酮是一种非常有效的中枢神经系统兴奋剂，其刺激作用似乎至少部分通过多巴胺能机制产生。
