Lipartiti M, Lazzaro A, Manev H
Fidia Research Laboratories, Abano Terme (PD), Italy.
Neuroreport. 1992 Oct;3(10):919-21. doi: 10.1097/00001756-199210000-00025.
The semisynthetic ganglioside derivative LIGA20 (II3Neu5-AcGgOse4-2-d-erythro-1,3-dihydroxy-2-dichloro-ac eta mide-4-trans-octadacene) was found to be about ten times more potent than the natural ganglioside GM1 in protecting neurones in culture against glutamate toxicity. Here we show that, in vivo, LIGA20 attenuated toxicity of the glutamate receptor agonist N-methyl-D-aspartate (NMDA). In seven-day-old rats NMDA was injected intracerebroventricularly, while LIGA20 or GM1 were administered subcutaneously. The loss in brain weight, five days following treatment, was used to estimate NMDA toxicity. Significant protection was observed with 2.5 mg kg-1 of LIGA20, while at least ten times this dose was needed for GM1, thus suggesting the superior in vivo pharmacological action of LIGA20.
半合成神经节苷脂衍生物LIGA20（II3Neu5 - AcGgOse4 - 2 - d - 赤藓糖 - 1,3 - 二羟基 - 2 - 二氯 - 乙酰胺 - 4 - 反式 - 十八碳二烯）在保护培养的神经元免受谷氨酸毒性方面，其效力约为天然神经节苷脂GM1的十倍。在此我们表明，在体内，LIGA20可减轻谷氨酸受体激动剂N - 甲基 - D - 天冬氨酸（NMDA）的毒性。在7日龄大鼠中，将NMDA脑室内注射，同时皮下给予LIGA20或GM1。治疗后5天的脑重量损失用于评估NMDA毒性。2.5 mg kg-1的LIGA20可观察到显著的保护作用，而GM1则需要至少十倍于此的剂量，这表明LIGA20在体内具有更优的药理作用。
