FURTHER EVIDENCE FOR AN AMPHETAMINE-LIKE MECHANISM OF ACTION OF THE ALKALOID CATHINONE
FURTHER EVIDENCE FOR AN AMPHETAMINE-LIKE MECHANISM OF ACTION OF THE ALKALOID CATHINONE
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DOI：
10.1016/0006-2952(86)90380-1
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发表时间：
1986-09-15
影响因子：
5.8
通讯作者：
GLENNON, RA
中科院分区：
文献类型：
--
作者：
KALIX, P;GLENNON, RA
生物碱（-）卡西酮是一种强效兴奋剂，其药理学性质与（+）安非他明非常相似。由于（-）卡西酮能够诱导生理性儿茶酚胺储存部位的释放，因此有人认为（-）卡西酮和（+）安非他明具有相同的作用机制。在本研究中，（-）卡西酮在诱导释放放射性从3 H-多巴胺预标记的大鼠尾状核组织的效力进行了比较，几个结构类似物，即其他四个氨基苯酮。发现（-）卡西酮是研究中最有效的化合物，其中只有去甲基卡西酮具有与（-）卡西酮相同数量级的作用。此外，（-）卡西酮及其两种类似物在行为实验中评估了它们在训练区分（+）安非他明和盐水的大鼠中替代（+）安非他明的能力。研究发现，与其他氨基甲酮不同，（-）卡西酮能够产生（+）安非他明样刺激作用，氟哌啶醇可以剂量相关方式拮抗这些作用。综上所述，这些发现支持了（+）安非他明和（-）卡西酮通过相同的多巴胺能机制产生中枢兴奋作用的假设。
The alkaloid (-)cathinone is a potent stimulant with pharmacological properties closely resembling those of (+)amphetamine. Since (-)cathinone is capable of inducing release at physiological catecholamine storage sites, it has been suggested that (-)cathinone and (+)amphetamine have the same mechanism of action. In the present study, the potency of (-)cathinone in inducing the release of radioactivity from 3H-dopamine prelabelled tissue of the rat caudate nucleus was compared to that of several structural analogs, i.e. to that of four other aminophenones. (-)Cathinone was found to be the most potent of the compounds under investigation, and among these only demethylcathinone had an effect that was within the same order of magnitude as that of (-)cathinone. Furthermore, (-)cathinone and two of its analogs were evaluated in behavioral experiments with regard to their ability to substitute for (+)amphetamine in rats trained to discriminate between (+)amphetamine and saline. It was found that, unlike the other aminophenones, (-)cathinone is capable of producing (+)amphetamine-like stimulus effects, and these can be antagonized by haloperidol in a dose-related manner. Taken together, these findings support the hypothesis that (+)amphetamine and (-)cathinone produce their central stimulant effect via the same dopaminergic mechanism.