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Peptides having glutamate release inhibitory activity and calcium channel inhibitory activity

机译:具有谷氨酸释放抑制活性和钙通道抑制活性的肽

摘要

PURPOSE:To provide a new peptide isolated from a venom originated from a spider called FTX, having a specific amino acid sequence, exhibiting a glutamic acid release-inhibiting activity and a calcium channel-inhibiting activity, and useful for preventing and treating agents for cerebral nervous diseases, etc. CONSTITUTION:The venom of a spider called FTX is acidified with 1% trifluoroacetic acid and subsequently subjected to a high performance liquid chromatography for allowing a hydrophobic group-modified silica gel carrier to adsorb an active fraction. The adsorbed active fraction is eluted with a hydrophilic organic solvent having a concentration gradient and subsequently collected to obtain the objective new peptide containing amino acid sequences of formulas I and II, having a glutamic acid release-inhibiting activity and/or a calcium channel-inhibiting activity, and useful as an agent for preventing and treating acute cerebral disorders generated in pathologic states such as cerebral ischemia and status epilepticus or cerebral nervous diseases such as Alzheimer's diseases and Huntington's chorea.
机译:目的:提供一种新的肽,该肽从称为FTX的蜘蛛的毒液中分离出来,具有特定的氨基酸序列,具有抑制谷氨酸释放的活性和抑制钙通道的活性,可用于预防和治疗脑部疾病的药物组成:一种叫做FTX的蜘蛛的毒液用1%三氟乙酸酸化,然后进行高效液相色谱分析,以使疏水基团改性的硅胶载体吸附活性组分。吸附的活​​性级分用具有浓度梯度的亲水性有机溶剂洗脱,然后收集以获得具有式I和II的氨基酸序列的,具有抑制谷氨酸释放活性和/或抑制钙通道的目标新肽。活性,并可用作预防和治疗在病理状态(例如脑缺血和癫痫持续状态)或脑神经疾病(例如阿尔茨海默氏病和亨廷顿舞蹈病)中产生的急性脑疾病的药物。

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