Nefiracetam is a

nootropic Nootropics ( or ) (colloquially brain supplements, smart drugs, cognitive enhancers, memory enhancers, or brain boosters) are chemical substances which purportedly improve cognitive functions, such as attention, memory, wakefulness, and self ...

drug of the racetam family. Preliminary research suggests that it may possess certain antidementia properties in rats.

Effects

Nefiracetam's cytoprotective actions are mediated by enhancement of

GABAergic In molecular biology and physiology, something is GABAergic or GABAnergic if it pertains to or affects the neurotransmitter gamma-aminobutyric acid (GABA). For example, a synapse is GABAergic if it uses GABA as its neurotransmitter, and a GABAergic ...

cholinergic Cholinergic agents are compounds which mimic the action of acetylcholine and/or butyrylcholine. In general, the word " choline" describes the various quaternary ammonium salts containing the ''N'',''N'',''N''-trimethylethanolammonium cation ...

, and monoaminergic neuronal systems. Preliminary studies suggest that it improves apathy and motivation in post-stroke patients. It may also exhibit antiamnesia effects for the Alzheimer's type and cerebrovascular type of dementia. In addition, research in animal models suggests antiamnesic effects against a number of memory impairing substances, including: ethanol, chlorodiazepoxide, scopolamine, bicuculline, picrotoxin, and cycloheximide.

Pharmacology

Unlike other racetams, nefiracetam shows high

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for the GABA_A receptor ( IC₅₀) = 8.5 nM), where it is presumed to be an

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

. 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. Nefiracetam is able to reverse the

amnesia Amnesia is a deficit in memory caused by brain damage or brain diseases,Gazzaniga, M., Ivry, R., & Mangun, G. (2009) Cognitive Neuroscience: The biology of the mind. New York: W.W. Norton & Company. but it can also be temporarily caused by t ...

caused by the GABA_A receptor antagonists picrotoxin and bicuculline in mice, although it failed to prevent

seizure A seizure is a sudden, brief disruption of brain activity caused by abnormal, excessive, or synchronous neuronal firing. Depending on the regions of the brain involved, seizures can lead to changes in movement, sensation, behavior, awareness, o ...

s induced by these drugs.

Concerns

Studies of long-term consumption of nefiracetam in humans and primates have shown it to have no toxicity. However, animals which metabolize nefiracetam differently from humans and primates are at risk for renal and testicular toxicity. Dogs especially are particularly sensitive, which has been shown to be caused by a specific metabolite, M-18 which isn't formed in humans. Higher doses than those in dogs were needed to cause testicular toxicity in rats, although no toxicity was seen in monkeys. Additionally, there has been no evidence of toxicity during clinical trials.

References

{{GABAA receptor modulators Racetams Acetanilides GABAA receptor agonists

Effects

Pharmacology

Concerns

See also

References