4-甲基氨基雷克斯的立体异构体的奖励性质：多巴胺系统的参与。,Pharmacology Biochemistry and Behavior

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4-甲基氨基雷克斯的立体异构体的奖励性质：多巴胺系统的参与。
Pharmacology Biochemistry and Behavior ( IF 3.3 ) Pub Date : 2005-06-29 , DOI: 10.1016/j.pbb.2005.04.020
Esa Meririnne ₁ , Miina Kajos , Aino Kankaanpää , Meri Koistinen , Kalervo Kiianmaa , Timo Seppälä

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4-Methylaminorex是一种潜在的滥用精神刺激药物，以四种立体异构体的形式存在：cis-4R，5S，cis-4S，5R，trans-4S，5S和trans-4R，5R。在非法样品中已经遇到了顺式异构体的外消旋混合物，但先前的动物研究表明，反式异构体也可能具有类似的兴奋剂样性质。我们测试了立体异构体是否具有奖励特性，并使用条件位置偏好法在大鼠中比较了它们的效能。此外，通过全身给药的多巴胺D1-和D2-受体拮抗剂SCH 23390和雷洛必利，或将神经毒素6-羟基多巴胺注射到伏隔核中，测试了脑中多巴胺能系统参与4-甲基氨基雷克斯奖励。所有四种异构体均引起位置偏爱，在效能上没有明显差异。SCH 23990和雷氯必利减弱了4-甲基氨基雷克斯诱导的位置偏好的增加，并且6-羟基多巴胺也趋于有效。这些发现表明4-甲基氨基雷克斯的所有四种立体异构体都具有有益的特性，因此具有滥用的可能性。反式异构体至少与顺式异构体一样有效。此外，脑多巴胺能系统似乎参与了4-甲基氨基雷克斯的奖励。

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Rewarding properties of the stereoisomers of 4-methylaminorex: involvement of the dopamine system.

4-Methylaminorex is a potential psychostimulant drug of abuse that exists as four stereoisomers: cis-4R,5S, cis-4S,5R, trans-4S,5S, and trans-4R,5R. The racemic mixture of the cis-isomers has been encountered in illicit samples, but previous animal studies suggest that also the trans-isomers could have similar stimulant-like properties. We tested whether the stereoisomers possess rewarding properties and compared their potency using the conditioned place preference method in rats. Furthermore, the involvement of the brain dopaminergic system in the 4-methylaminorex reward was tested with the dopamine D1- and D2-receptor antagonists SCH 23390 and raclopride administered systemically, or with the neurotoxin 6-hydroxydopamine injected into the nucleus accumbens. All the four isomers induced place preference, with no apparent differences in their potency. SCH 23990 and raclopride attenuated 4-methylaminorex-induced increase in place preference, and 6-hydroxydopamine also tended to be efficacious. These findings indicate that all the four stereoisomers of 4-methylaminorex possess rewarding properties and thus abuse potential; the trans-isomers are at least as potent as the cis-isomers. Furthermore, the brain dopaminergic system appears to be involved in the 4-methylaminorex-reward.

更新日期：2019-11-01

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