Nefiracetam

Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca²⁺ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research^{[1][2][3][4][5][6]}. In Vitro:Nefiracetam (1-1000 nM, 10-60 min) increases rat dentate gyrus hippocampal neurotransmission (250%) in a dose-dependent manner^[1].
Nefiracetam (1 μM, 20 min) enhances the activity of neuronal nAChR α3β2 (127%), α3β4 (124%), α4β2 (129%), α4β4 (112%), and α7 (178%) receptors in Xenopus oocytes^[1].
Nefiracetam (1-1000 nM) improves NMDA receptor-dependent long-term potentiation (LTP) (64%) in the CA1 region of the hippocampus of OBX mice^[2].
Nefiracetam (10 nM) enhances the autophosphorylation of CaMKIIα (Thr286) (77.3%) and PKCα (Ser657) (93.3%) in the CA1 region of the hippocampus of OBX mice^[2].
Nefiracetam (1 μM) increases Ca²⁺ currents flowing through high voltage-activated (N/L-type) calcium channels in NG108-15 cells (more than 2 fold)^[6].
In Vivo:Nefiracetam (0.1-1.0 mg/kg, p.o.) improves spatial reference memory-related behaviors in olfactory bulbectomized (OBX) mice^[2].
Nefiracetam (10 mg/kg, i.g., once a day for 3-5 days) increases the GABA content in the right hippocampus of rats with microsphere embolization^[4].
Nefiracetam (10 mg/kg, i.g., once a day for 3-5 days) increases the glutamate decarboxylase activity in the right cerebral cortex and hippocampus of rats with microsphere embolization^[4].
Nefiracetam (10 mg/kg, p.o., once) inhibits Ro 5-4864 (PBR activator)-induced convulsions in EL (Epilepsy-prone Lesion) mice in a dose-dependent manner (ED₅₀: 17.2 mg/kg) ^[5].
Nefiracetam (10 mg/kg, p.o., once) inhibits Ro 5-4864-induced convulsions in DDY mice (parental strain of EL mice) and spontaneous epilepsy in EL mice in a dose-dependent manner^[5].