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Nefiracetam 77191-36-7

Product Description

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Molecular Weight:

246.3 Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.

Biological Activity

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.


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.

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Product Categories : Transmembrane Transporters > GABA Receptor Inhibitor