同义名 :	DZL-221; DM9384
	CAS号 :	77191-36-7
	货号 :	A517196
	分子式 :	C14H18N2O2
	纯度 :	97%
	分子量 :	246.3
	MDL号 :	MFCD00209882
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Nefiracetam enhances neuronal systems related to GABAergic, cholinergic, and monoaminergic pathways and is used to manage Ro 5-4864-induced convulsions. It targets the GABA Receptor. At submicromolar concentrations (0.01-0.1 μM), Nefiracetam leads to a short-term reduction of ACh-evoked currents, decreasing them to 30% and 38% of the baseline after a 10-minute exposure, respectively. At higher micromolar concentrations (1-10 μM), it causes a long-term enhancement of these currents. This interaction with PKA and PKC pathways might explain the cellular mechanisms underlying the cognitive enhancement provided by Nefiracetam[1]. Orally administered, Nefiracetam prevents Ro 5-4864-induced convulsions in EL and DDY mice, particularly at doses exceeding 10 mg/kg[2]. Administering Nefiracetam 1 hour prior to each training session on a daily basis enhances the learning of the avoidance behavior [3].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	4.06mL 0.81mL 0.41mL	20.30mL 4.06mL 2.03mL	40.60mL 8.12mL 4.06mL

参考文献

[1]Nishizaki, T., et al., Nefiracetam modulates acetylcholine receptor currents via two different signal transduction pathways. Mol Pharmacol, 1998. 53(1): p. 1-5. [2]Shiotani, T., et al., Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors. Brain Res, 2000. 859(2): p. 255-61. [3]Sakurai, T., et al., Effects of N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide (DM-9384) on learning and memory in rats. Jpn J Pharmacol, 1989. 50(1): p. 47-53.