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首页> 外文期刊>The Journal of toxicological sciences >New recreational drug 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (alpha-PVP) activates central nervous system via dopaminergic neuron
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New recreational drug 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (alpha-PVP) activates central nervous system via dopaminergic neuron

机译：新的休闲药物1-苯基-2-（1-吡咯烷基）-1-戊酮（α-PVP）通过多巴胺能神经元激活中枢神经系统

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摘要

1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (α-PVP) is a new designer drug of the cathinone type. People who have taken drugs containing α-PVP or other synthetic cathinone reportedly lose consciousness, develop difficulty breathing, and at worst case, die. However, the mechanism underlying α-PVP-induced neurotoxicity is unknown. The objective of the present study was to investigate the effect of α-PVP on the central nervous system (CNS) and compare its neurotoxicity with that of methamphetamine (METH) in mice. Balb/c male mice (8 weeks old) were orally administered α-PVP (25 mg/ kg) or METH (5 mg/kg). α-PVP induced a significant increase in locomotor activity, which occurred earlier than locomotor activity induced by METH. This increase was inhibited by the D1 receptor antagonist SCH23990 (50 μg/kg, i.p.) and the D2 receptor antagonist sulpiride (50 mg/kg, i.m.). The extracellular concentration of dopamine (DA) in the striatum, determined by in vivo microdialysis increased immediately after α-PVP administration. These results suggest that α-PVP stimulates DA release, causing an increase in locomotor activity, and that this stimulatory effect of α-PVP on CNS is mediated, at least in part, by the D1 and D2 receptors.
机译：1-苯基-2-（1-吡咯烷基）-1-戊酮（α-PVP）是Cathinone类型的新型设计药物。据报道，服用含α-PVP或其他合成卡西酮的药物的人会失去知觉，呼吸困难，甚至死亡。但是，尚不清楚α-PVP诱导的神经毒性的潜在机制。本研究的目的是研究α-PVP对中枢神经系统（CNS）的影响，并将其与小鼠甲基苯丙胺（METH）的神经毒性进行比较。 Balb / c雄性小鼠（8周大）口服给予α-PVP（25 mg / kg）或METH（5 mg / kg）。 α-PVP引起的运动活动显着增加，发生时间比METH引起的运动活动更早。这种增加被D1受体拮抗剂SCH23990（50μg/ kg，i.p.）和D2受体拮抗剂舒必利（50 mg / kg，i.m.）抑制。通过体内微透析测定，纹状体中多巴胺（DA）的细胞外浓度在施用α-PVP后立即增加。这些结果表明，α-PVP刺激DA释放，引起运动活性增加，并且α-PVP对CNS的这种刺激作用至少部分地由D1和D2受体介导。

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