中文名：奈非西坦
英文名：Nefiracetam
英文別名：DZL 221;N-?(2,?6-?dimethylphenyl)?-?2-?oxo-1-?pyrrolidineacetamide
純度：10mM in DMSO
貨號：N408557
包裝：1ml
Cas號：77191-36-7
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
In?vitro
Nefiracetam at a concentration of 1 μM increases a long-lasting component of calcium channel currents two-fold without affecting a transient component. Nefiracetam 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. In primary cultures of rat hippocampal neurons, nefiracetam increases the rate of nicotine-sensitive miniature excitatory postsynaptic currents. Nefiracetam induces a long-lasting facilitation of synaptic transmission in both the CA1 area and the dentate gyrus of rat hippocampal slices, and the facilitation is inhibited by α-bungarotoxin and mecamylamine. Nefiracetam enhances activity of nicotinic ACh receptors by interacting with a PKC pathway, thereby increasing glutamate release from presynaptic terminals, and then leading to a sustained facilitation of hippocampal neurotransmission.
In?vivo
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. Nefiracetam administered daily 1 hour before each training session facilitates the acquisition process of the avoidance response.
Cell?Data
cell?lines：HCC827, H3255, HCC827 GR, H1975, PC9, PC9 GR, Calu-3, H1819, and Ba/F3
Concentrations：~1 μM
Incubation?Time：24 hours - 48 hours
Powder?Purity:≥100%
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關(guān)鍵字： DZL 221;N-?(2,?6-?dimethylphenyl)?-?2-?oxo-1-?pyrrolidineacetamide
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