Lopez C M, Govoni S, Battaini F, Bergamaschi S, Longoni A, Giaroni C, Trabucchi M
Institute of Pharmacological Sciences, University of Milan, Italy.
Pharmacol Biochem Behav. 1991 Aug;39(4):835-40. doi: 10.1016/0091-3057(91)90040-9.
The present study investigates the effect of the administration of alpha-glycerylphosphorylcholine (alpha-GPC) on scopolamine-induced amnesia and on brain acetylcholine (ACh) levels and release in rats. The results indicate that alpha-GPC, when administered orally, reverses the amnesia caused by scopolamine in passive avoidance. The peak effect is observed using 600 mg/kg IG, 5 h before training. The effect of the drug is long lasting (up 30 h) in accordance with its pharmacokinetic characteristics. Since, alpha-GPC administered IG is cleaved within the gut mucosal cells to glycerophosphate and free choline, it is tempting to speculate that this drug acts by increasing the ACh precursor pool. This view is supported also by the observation that alpha-GPC partially counteracts the decrease of brain ACh levels elicited by scopolamine administration. The effect is observed in the hippocampus and cortex, but not in the striatum. Moreover, in ex vivo experiments, alpha-GPC is able to increase the amount of ACh released by rat hippocampus slices following potassium stimulation.
本研究调查了α-甘油磷酸胆碱（α-GPC）给药对东莨菪碱诱导的大鼠失忆以及对大鼠脑内乙酰胆碱（ACh）水平和释放的影响。结果表明，口服α-GPC可逆转东莨菪碱在被动回避实验中引起的失忆。在训练前5小时给予600mg/kg灌胃给药时观察到峰值效应。根据其药代动力学特性，该药物的作用持久（长达30小时）。由于灌胃给予的α-GPC在肠粘膜细胞内被裂解为甘油磷酸和游离胆碱，因此很容易推测该药物通过增加ACh前体池起作用。东莨菪碱给药引起脑内ACh水平下降，α-GPC能部分对抗这一现象，这一观察结果也支持了这一观点。在海马体和皮质中观察到了这种效应，但在纹状体中未观察到。此外，在体外实验中，α-GPC能够增加钾刺激后大鼠海马体切片释放的ACh量。
