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Discriminative stimulus properties of (-)ephedrine.

机译:(-)麻黄碱的鉴别刺激特性。

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Ephedrine, a structural analog of methamphetamine, is one of the major constituents of legally available herbal dietary supplements. Although racemic ephedrine and ephedra extract have been previously used as training drugs in drug discrimination studies, there is evidence that the two optical isomers of ephedrine do not produce identical amphetamine-like stimulus effects in rats. Consequently, we trained a group of six male Sprague-Dawley rats to discriminate 4 mg/kg of the more potent optical isomer of ephedrine, (-)ephedrine, from saline vehicle. The (-)ephedrine stimulus (ED50 = 0.8 mg/kg) generalized to other central stimulants such as S(+)amphetamine (ED50 = 0.4 mg/kg), cocaine (ED50 = 2.7 mg/kg), methylphenidate (ED50 = 1.2 mg/kg), S(-)methcathinone (ED50 = 0.3 mg/kg), and caffeine (ED50 = 36.7 mg/kg), but stimulus generalization failed to occur to either S(+)methamphetamine or N-methyl-1-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA). In addition, although we have previously shown that a (+)amphetamine stimulus generalizes to (-)ephedrine but not to (+)ephedrine, in the present investigation the (-)ephedrine stimulus generalized to (+)ephedrine (ED50 = 2.6 mg/kg). From the findings (a) that (-)ephedrine is approximately 10 times less potent than (+)amphetamine in (+)amphetamine-trained rats, whereas it is only half as potent as (+)amphetamine in (-)ephedrine-trained animals; (b) that the (-)ephedrine stimulus failed to generalize to (+)methamphetamine; and (c) that the (-)ephedrine stimulus generalized to (+)ephedrine, it is concluded that the stimulus effects of (+)amphetamine and (-)ephedrine as training drugs, while similar, are not identical. It is also concluded that the stimulus effects of (-)ephedrine and those of the designer drug MDMA, while perhaps sharing some amphetaminergic commonality, are nonidentical.
机译:麻黄碱是一种甲基苯丙胺的结构类似物,是合法可得的草药膳食补充剂的主要成分之一。尽管消旋麻黄碱和麻黄提取物以前曾在药物鉴别研究中用作训练药物,但有证据表明麻黄碱的两种光学异构体在大鼠中不会产生相同的苯丙胺样刺激作用。因此,我们训练了一组六只雄性Sprague-Dawley大鼠,以从盐水媒介物中区分出4 mg / kg的麻黄碱(-)麻黄碱更有效的光学异构体。 (-)麻黄碱刺激(ED50 = 0.8 mg / kg)普遍适用于其他中枢兴奋剂,例如S(+)苯丙胺(ED50 = 0.4 mg / kg),可卡因(ED50 = 2.7 mg / kg),哌醋甲酯(ED50 = 1.2 mg / kg),S(-)甲卡西酮(ED50 = 0.3 mg / kg)和咖啡因(ED50 = 36.7 mg / kg),但对S(+)methamphetamine或N-methyl-1-刺激均未发生(3,4-亚甲基二氧苯基)-2-氨基丙烷(MDMA)。此外,尽管我们先前已经证明(+)苯丙胺刺激剂普遍适用于(-)麻黄碱,但不能适用于(+)麻黄碱,但在本研究中,(-)麻黄碱刺激适用于(+)麻黄碱(ED50 = 2.6 mg /公斤)。根据发现(a),(-)麻黄碱在(+)苯丙胺训练的大鼠中的效力比(+)苯丙胺约低10倍,而其效力仅为(-)麻黄碱训练的(+)苯丙胺的一半动物; (b)(-)麻黄碱刺激未能推广到(+)甲基苯丙胺; (c)(-)麻黄碱刺激泛化为(+)麻黄碱,得出的结论是(+)苯丙胺和(-)麻黄碱作为训练药物的刺激作用虽然相似,但并不相同。还得出结论,(-)麻黄碱和设计药物MDMA的刺激作用虽然可能具有一些苯丙胺能的共同性,但并不相同。

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