Nefiracetam

Nefiracetam is a nootropic drug of the racetam family. Preliminary research suggests that it may possess certain antidementia properties in rats.^[2]

Nefiracetam

Clinical data
Routes of administration	Oral
ATC code	none
Legal status
Legal status	AU: S4 (Prescription only) US: Unscheduled
Pharmacokinetic data
Elimination half-life	3-5 hours[1]
Identifiers
IUPAC name N-(2,6-dimethylphenyl)-2-(2-oxopyrrolidin-1-yl)acetamide
CAS Number	77191-36-7 N
PubChem CID	71157
ChemSpider	64299 Y
UNII	1JK12GX30N
ChEMBL	ChEMBL260829 Y
CompTox Dashboard (EPA)	DTXSID2020923
ECHA InfoCard	100.163.910
Chemical and physical data
Formula	C14H18N2O2
Molar mass	246.310 g·mol−1
3D model (JSmol)	Interactive image
SMILES O=C2N(CC(=O)Nc1c(cccc1C)C)CCC2
InChI InChI=1S/C14H18N2O2/c1-10-5-3-6-11(2)14(10)15-12(17)9-16-8-4-7-13(16)18/h3,5-6H,4,7-9H2,1-2H3,(H,15,17) Y Key:NGHTXZCKLWZPGK-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Effects

Nefiracetam's cytoprotective actions are mediated by enhancement of GABAergic, cholinergic, and monoaminergic neuronal systems.^{[citation needed]} 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.^[3][4] In addition, research in animal models suggests antiamnesic effects against a number of memory impairing substances, including: ethanol, chlorodiazepoxide, scopolamine, bicuculline, picrotoxin, and cycloheximide.^[5]

Pharmacology

Unlike other racetams, nefiracetam shows high affinity for the GABA_A receptor (IC₅₀) = 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.^[6][7] Nefiracetam is able to reverse the amnesia caused by the GABA_A receptor antagonists picrotoxin and bicuculline in mice, although it failed to prevent seizures induced by these drugs.^[7]

Concerns

Studies of long-term consumption of nefiracetam in humans and primates have shown it to have no toxicity.^[8][9] However, animals which metabolize nefiracetam differently from humans and primates are at risk for renal and testicular^[10][11] 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.^[12] 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.^[8][9]

See also

• Racetams
• Guvacine
• Phenibut