Goldsmith Robert, Aburahma Amal, Sprague Jon E
The Ohio Attorney General's Center for the Future of Forensic Science, Bowling Green State University, Bowling Green, OH 43403, USA.
Brain Sci. 2024 Mar 8;14(3):265. doi: 10.3390/brainsci14030265.
Structural modifications to synthetic psychoactive cathinones (SPCs), a class of drugs that contain a β-keto modification of the phenethylamine pharmacophore of amphetamine, induce differences in dopamine transporter (DAT) activity. Here, in vivo retrodialysis was utilized to deliver the SPCs 3,4-methylenedioxypyrovalerone (MDPV, a DAT inhibitor) or methylone (a DAT substrate) into the caudate putamen of male Sprague-Dawley rats. Dialysate samples were collected prior to and post drug administration, and temporal changes in dopamine concentration were quantified using HPLC-EC methods. Methylone elicited a 200% increase and MDPV a 470% increase in dopamine levels at the 10 min time point. The findings demonstrate that in vivo retrodialysis can be used to evaluate the effects of SPCs on neurotransmission in the brain.
合成卡西酮(SPCs)是一类药物,其对苯丙胺的苯乙胺药效基团进行了β-酮修饰,结构修饰会导致多巴胺转运体(DAT)活性产生差异。在此,利用体内逆向透析法将SPCs 3,4-亚甲基二氧吡咯戊酮(MDPV,一种DAT抑制剂)或甲酮(一种DAT底物)注入雄性Sprague-Dawley大鼠的尾状壳核。在给药前和给药后收集透析液样本,并使用高效液相色谱-电化学检测法对多巴胺浓度的时间变化进行定量分析。在10分钟时间点,甲酮使多巴胺水平升高了200%,MDPV使多巴胺水平升高了470%。这些研究结果表明,体内逆向透析法可用于评估SPCs对大脑神经传递的影响。