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Aniracetam (brand names Draganon, Sarpul, Ampamet, Memodrin, Referan), also known as N-anisoyl-2-pyrrolidinone, is a racetam which is sold in Europe as a prescription drug. It is not approved by the Food and Drug Administration for use in the United States as a prescription medication or dietary supplement .
Like some ampakines, some racetams, such as piracetam and aniracetam, are positive allosteric modulators of the AMPA receptor. [7] Racetams are understood to work by allosterically modulating glutamate receptors, specifically AMPA receptors, leading to Ca 2+ influx that is excitatory. [8]
Oxiracetam is well absorbed from the gastrointestinal tract with a bioavailability of 56-82%. [6] Peak serum levels are reached within one to three hours after a single 800 mg or 2000 mg oral dose, with the maximal serum concentration reaching between 19 and 31 μg/ml at these doses.
The racetams have poorly understood mechanisms, although piracetam and aniracetam are known to act as positive allosteric modulators of AMPA receptors and appear to modulate cholinergic systems. [33] Similar compounds, such as noopept and aloracetam , do not meet the chemical definition for being a racetam, though they are considered "racetam ...
Unlike other racetams, nefiracetam shows high affinity for the GABA A receptor (IC 50) = 8.5 nM), where it is presumed to be an agonist. [6] [7] It was able to potently inhibit 80% of muscimol binding to the GABA A receptor, although it failed to displace the remaining 20% of specific muscimol binding.
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AMPA receptors modulated by aniracetam and CX614 will deactivate slower, and facilitate more overall cation transport. This is likely accomplished by aniracetam or CX614 binding to the back of the "clam shell" that contains the binding site for glutamate, stabilizing the closed conformation associated with activation of the AMPA receptor. [5] [9]