Background:

Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal systems enhancer for Ro 5-4864-induced convulsions.Target: GABA ReceptorNefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01-0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1-10 μM). Nefiracetam interacts with PKA and PKC pathways, which may explain a cellular mechanism for the action of cognition-enhancing agents. Lower (submicromolar) concentrations of the nootropic Nefiracetam reduces ACh-evoked currents to 30% (0.01 μM) and 38% (0.1 μM) of control after a 10-minute treatment [1].Nefiracetam administered orally inhibits Ro 5-4864-induced convulsions in EL mice. Nefiracetam also efficiently inhibits Ro 5-4864-induced convulsions in DDY mice at doses higher than 10 mg/kg [2]. Nefiracetam administered daily 1 hour before each training session facilitates the acquisition process of the avoidance response [3].

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.