Trabucchi M, Govoni S, Battaini F
Farmaco Sci. 1986 Apr;41(4):325-34.
The present study investigates the cholinomimetic properties of the drug L-alpha-glycerylphosphorylcholine (alpha-GPC) at CNS level. Experiments using tritium labelled alpha-GPC indicate that the drug reaches the brain after i.p. and per os administration. In order to study the cholinomimetic properties of this drug an indirect functional index of cholinergic activation was used. In fact cholinergic agonists induce an activation of striatal dopaminergic output. alpha-GPC both i.p. and per os administered increased striatal dihydroxyphenylacetic acid (DOPAC) content. In addition, the in vitro K+ stimulated dopamine release was increased in rats treated in vivo with alpha-GPC. Since alpha-GPC has a weak displacing activity in QNB binding, the in vivo cholinergic activity might be due to the fact that this drug may increase the availability of choline for acetylcholine synthesis leading to increased acetylcholine production. This activity may be useful in those situations such as aging in which cholinergic activity is deficient.
本研究在中枢神经系统水平研究了药物L-α-甘油磷酰胆碱(α-GPC)的拟胆碱特性。使用氚标记的α-GPC进行的实验表明,该药物经腹腔注射和口服给药后可到达大脑。为了研究该药物的拟胆碱特性,使用了胆碱能激活的间接功能指标。事实上,胆碱能激动剂可诱导纹状体多巴胺能输出的激活。腹腔注射和口服α-GPC均增加了纹状体二羟基苯乙酸(DOPAC)的含量。此外,用α-GPC进行体内治疗的大鼠,体外钾离子刺激的多巴胺释放增加。由于α-GPC在QNB结合中具有较弱的置换活性,体内胆碱能活性可能是由于该药物可能增加胆碱用于乙酰胆碱合成的可用性,从而导致乙酰胆碱产量增加。这种活性在胆碱能活性不足的情况下(如衰老)可能是有用的。