A novel psychoactive substance, α-pyrrolidinopentiothiophenone (α-PVT), is a structural analog to amphetamine. Recently, it has been shown that α-PVT has an abuse potential similar to psychomotor stimulants like cocaine or amphetamine. However, it has not been performed yet to determine whether α-PVT develops behavioral sensitization, a well-known phenomenon for psychomotor stimulants. In the present study, rats were first pre-exposed to either saline or α-PVT (20 mg/kg, IP) with a total of four injections in every 2-3 days of interval. Then, 2-weeks after withdrawal, locomotor activity was measured with a challenge dose (10 mg/kg, IP) of α-PVT and the nucleus accumbens core region was taken out. Similar to psychomotor stimulants, repeated administration of α-PVT produced locomotor sensitization. Further, the phosphorylation levels of GSK3β in the nucleus accumbens core were found to be decreased only in rats with sensitization developed, but not in those with acute or non-sensitized. Correlation analysis revealed that the phosphorylation levels of GSK3β have a strong negative correlation with locomotor activity only in rats with α-PVT pre-exposed, but not in those with its acute injection. These results suggest that a certain level of change in the phosphorylation levels of GSK3β in the nucleus accumbens core may involve in mediating the expression of locomotor sensitization by repeated injection of α-PVT in rats.

中文翻译：

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一种新型的合成卡西酮，α-吡咯烷基戊噻吩酮（PVT）在大鼠中产生运动性敏化：伏伏核核心中GSK3β连接的意义。

一种新型的精神活性物质，α-吡咯烷基戊二噻吩酮（α-PVT），是苯丙胺的结构类似物。最近，已经显示出α-PVT具有类似于精神运动兴奋剂如可卡因或苯丙胺的滥用潜力。但是，尚未确定α-PVT是否发展出行为敏化作用，这是精神运动兴奋剂的一种众所周知的现象。在本研究中，首先将大鼠预先暴露于盐水或α-PVT（20 mg / kg，IP）中，每2-3天间隔注射四次。然后，在停药后2周，用α-PVT的攻击剂量（10mg / kg，IP）测量运动活性，并取出伏隔核核心区。与精神运动兴奋剂相似，反复服用α-PVT会产生运动致敏作用。进一步，发现伏隔核核心中GSK3β的磷酸化水平仅在发育敏化的大鼠中降低，而在急性或未敏化的大鼠中没有降低。相关分析表明，仅在预先暴露于α-PVT的大鼠中，GSK3β的磷酸化水平与运动能力呈负相关，而在急性注射的大鼠中则没有。这些结果表明伏隔核中GSK3β的磷酸化水平的一定水平的改变可能涉及通过反复注射α-PVT在大鼠中介导运动敏化的表达。相关分析表明，仅在预先暴露于α-PVT的大鼠中，GSK3β的磷酸化水平与运动能力呈负相关，而在急性注射的大鼠中则没有。这些结果表明伏隔核核心中GSK3β的磷酸化水平的一定水平的改变可能涉及通过反复注射α-PVT在大鼠中介导运动敏化的表达。相关分析表明，仅在预先暴露于α-PVT的大鼠中，GSK3β的磷酸化水平与运动能力呈负相关，而在急性注射的大鼠中则没有。这些结果表明伏隔核中GSK3β的磷酸化水平的一定水平的改变可能涉及通过反复注射α-PVT在大鼠中介导运动敏化的表达。