School of Biomedical Sciences, University of Nottingham Medical School, Queen's Medical Centre, Nottingham, UK.
Br J Pharmacol. 2013 Feb;168(4):966-77. doi: 10.1111/j.1476-5381.2012.02236.x.
Recreational users report that mephedrone has similar psychoactive effects to 3,4-methylenedioxymethamphetamine (MDMA). MDMA induces well-characterized changes in body temperature due to complex monoaminergic effects on central thermoregulation, peripheral blood flow and thermogenesis, but there are little preclinical data on the acute effects of mephedrone or other synthetic cathinones.
The acute effects of cathinone, methcathinone and mephedrone on rectal and tail temperature were examined in individually housed rats, with MDMA included for comparison. Rats were killed 2 h post-injection and brain regions were collected for quantification of 5-HT, dopamine and major metabolites. Further studies examined the impact of selected α-adrenoceptor and dopamine receptor antagonists on mephedrone-induced changes in rectal temperature and plasma catecholamines.
At normal room temperature, MDMA caused sustained decreases in rectal and tail temperature. Mephedrone caused a transient decrease in rectal temperature, which was enhanced by α(1) -adrenoceptor and dopamine D(1) receptor blockade, and a prolonged decrease in tail temperature. Cathinone and methcathinone caused sustained increases in rectal temperature. MDMA decreased 5-HT and/or 5-hydroxyindoleacetic acid (5-HIAA) content in several brain regions and reduced striatal homovanillic acid (HVA) levels, whereas cathinone and methcathinone increased striatal HVA and 5-HIAA. Cathinone elevated striatal and hypothalamic 5-HT. Mephedrone elevated plasma noradrenaline levels, an effect prevented by α-adrenoceptor and dopamine receptor antagonists.
MDMA and cathinones have different effects on thermoregulation, and their acute effects on brain monoamines also differ. These findings suggest that the adverse effects of cathinones in humans cannot be extrapolated from previous observations on MDMA.
娱乐性使用者报告称，麦角酸二乙酰胺（MDA）具有类似的致幻作用。由于对中枢体温调节、外周血流和产热的复杂单胺能作用，MDMA 会引起体温的明显变化，但关于麦角酸二乙酰胺或其他合成卡西酮的急性影响，几乎没有临床前数据。
在单独饲养的大鼠中检查了卡西酮、甲卡西酮和麦角酸二乙酰胺对直肠和尾巴温度的急性影响，并包括 MDMA 进行比较。大鼠在注射后 2 小时被杀死，并收集大脑区域以定量 5-HT、多巴胺和主要代谢物。进一步的研究检查了选定的 α-肾上腺素能受体和多巴胺受体拮抗剂对麦角酸二乙酰胺引起的直肠温度和血浆儿茶酚胺变化的影响。
在正常室温下，MDMA 导致直肠和尾巴温度持续下降。麦角酸二乙酰胺引起直肠温度短暂下降，这一下降可通过 α(1) -肾上腺素能受体和多巴胺 D(1) 受体阻断增强，并导致尾巴温度持续下降。卡西酮和甲卡西酮引起直肠温度持续升高。MDMA 降低了几个脑区的 5-HT 和/或 5-羟吲哚乙酸（5-HIAA）含量，并降低了纹状体高香草酸（HVA）水平，而卡西酮和甲卡西酮增加了纹状体 HVA 和 5-HIAA。卡西酮升高了纹状体和下丘脑的 5-HT。麦角酸二乙酰胺升高了血浆去甲肾上腺素水平，这一作用可被 α-肾上腺素能受体和多巴胺受体拮抗剂阻止。
MDMA 和卡西酮对体温调节有不同的影响，它们对脑单胺的急性影响也不同。这些发现表明，不能从以前对 MDMA 的观察中推断卡西酮在人类中的不良影响。
