Nefiracetam Overview

Nefiracetam Research Summary

Nefiracetam (DM-9384) is a nootropic drug developed by Daiichi for the treatment of cerebrovascular disorders, including post-stroke symptoms and Alzheimer's-type dementia. As of 2000, the drug completed Phase II trials in the United States and clinical trials in China, with modified Phase III trials underway in Japan. Despite retraction of its Japanese NDA due to inadequate efficacy in February 2002, there were still projections for its approval and launch in late 2002 or 2003, with estimated sales growth in Japan.

Nefiracetam has shown potential in research for various pharmacological effects:

• Protective effects on neuronal cells against cell death caused by toxins affecting sodium and glutamate channels.
• Enhancement of synaptic transmission in the hippocampus via activation of protein kinase C (PKC) and increased glutamate release, indicating potential treatment for senile dementia and Alzheimer's disease.
• Facilitation of hippocampal neurotransmission through nicotinic acetylcholine receptors and a PKC-dependent pathway.
• Potentiation of NMDA receptor currents, suggesting mechanisms for cognitive improvement.
• Increase in acetylcholine release, potentially countering memory impairments in Alzheimer's disease.
• Enhancement of associative learning in older rabbits, indicating possible benefits for cognitive tasks impaired in Alzheimer's disease.
• Improvement of learning and memory in rats with post-ischemic seizures and brain injury.
• Antiepileptic properties based on its effects on post-ischemic nonconvulsive seizures in rats.
• Long-term enhancement of memory retention in older rabbits.

Nefiracetam has also been studied for its impact on specific receptors and neurotransmitters:

• Modulation of neuronal calcium channels, involved in memory-enhancing effects.
• Interaction with GABAergic and cholinergic systems in the brain.

The drug's efficacy, safety, and potential therapeutic uses continue to be explored in the context of neuroprotection, cognitive enhancement, and treatment of neurological disorders.

References:

1. Chromatographic behaviour predicts the ability of potential nootropics to permeate the blood-brain barrier
2. Nefiracetam. Daiichi Seiyaku
3. Antinociceptive effect of intrathecal loperamide: role of mu-opioid receptor and calcium channels
4. Nefiracetam attenuates post-ischemic nonconvulsive seizures in rats and protects neuronal cell death induced by veratridine and glutamate
5. The inhibitory guanine nucleotide-binding regulatory component of adenylate cyclase. Properties and function of the purified protein
6. Pyrrolidone derivatives
7. The anti-dementia drug nefiracetam facilitates hippocampal synaptic transmission by functionally targeting presynaptic nicotinic ACh receptors
8. Mechanisms of action of cognitive enhancers on neuroreceptors
9. Ion channel modulators that enhance acetylcholine release: potential therapies for Alzheimer's disease
10. Enhancement of neuronal calcium channel currents by the nootropic agent, nefiracetam (DM-9384), in NG108-15 cells
11. Possible involvement of the activation of voltage-sensitive calcium channels in the ameliorating effects of nefiracetam on scopolamine-induced impairment of performance in a passive avoidance task
12. Bryostatin-1 promotes long-term potentiation via activation of PKCα and PKCε in the hippocampus
13. Nefiracetam potentiates N-methyl-D-aspartate (NMDA) receptor function via protein kinase C activation and reduces magnesium block of NMDA receptor
14. CaM kinase II and protein kinase C activations mediate enhancement of long-term potentiation by nefiracetam in the rat hippocampal CA1 region
15. Phosphorylation of myristoylated alanine-rich protein kinase C substrate by mitogen-activated protein kinase in cultured rat hippocampal neurons following stimulation of glutamate receptors
16. Characterization of protein kinase A and protein kinase C phosphorylation of the N-methyl-D-aspartate receptor NR1 subunit using phosphorylation site-specific antibodies
17. Characterization of multiple phosphorylation sites on the AMPA receptor GluR1 subunit
18. Antagonistic effects of dopaminergic signaling and ethanol on protein kinase A-mediated phosphorylation of DARPP-32 and the NR1 subunit of the NMDA receptor
19. Nefiracetam activation of CaM kinase II and protein kinase C mediated by NMDA and metabotropic glutamate receptors in olfactory bulbectomized mice
20. New aspects of neurotransmitter release and exocytosis: dynamic and differential regulation of synapsin I phosphorylation by acute neuronal excitation in vivo
21. Pharmacological study on Alzheimer's drugs targeting calcium/calmodulin-dependent protein kinase II
22. Effects of DM-9384, a cyclic derivative of GABA, on amnesia and decreases in GABAA and muscarinic receptors induced by cycloheximide
23. Role of cholinergic and GABAergic neuronal systems in cycloheximide-induced amnesia in mice
24. Reversal effect of DM-9384 on scopolamine-induced acetylcholine depletion in certain regions of the mouse brain
25. Nefiracetam ameliorates associative learning impairment in the scopolamine-injected older rabbit
26. The long-term effects of nefiracetam on learning in older rabbits
27. Cholinergic septo-hippocampal innervation is required for trace eyeblink classical conditioning
28. Hippocampus in delay eyeblink classical conditioning: essential for nefiracetam amelioration of learning in older rabbits
29. Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist
30. Presynaptic nicotinic acetylcholine receptors as a functional target of nefiracetam in inducing a long-lasting facilitation of hippocampal neurotransmission
31. Nefiracetam facilitates hippocampal neurotransmission by a mechanism independent of the piracetam and aniracetam action
32. Nefiracetam and galantamine modulation of excitatory and inhibitory synaptic transmission via stimulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons
33. Nefiracetam elevates extracellular acetylcholine level in the frontal cortex of rats with cerebral cholinergic dysfunctions: an in vivo microdialysis study
35. Effects of nefiracetam on spatial memory function and acetylcholine and GABA metabolism in microsphere-embolized rats
36. Modulation of the neuronal nicotinic acetylcholine receptor-channel by the nootropic drug nefiracetam
37. Nootropic drug modulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons
38. Nefiracetam modulates acetylcholine receptor currents via two different signal transduction pathways
39. Nicotinic receptor activation in human cerebral cortical interneurons: a mechanism for inhibition and disinhibition of neuronal networks
40. Potentiation of N-methyl-D-aspartate-induced currents by the nootropic drug nefiracetam in rat cortical neurons
41. Protein kinase C reduces Mg2+ block of NMDA-receptor channels as a mechanism of modulation
42. A 'long-term-potentiation-like' facilitation of hippocampal synaptic transmission induced by the nootropic nefiracetam
43. Modulation of N-methyl-D-aspartate receptors by donepezil in rat cortical neurons
44. The role of glutamate neurotoxicity in hypoxic-ischemic neuronal death
45. The protective action of nefiracetam against electrophysiological and metabolic damage in the hippocampus after deprivation of glucose and oxygen
46. DM-9384, a new cognition-enhancing agent, increases the turnover of components of the GABAergic system in the rat cerebral cortex
47. Effects of DM-9384 in a model of amnesia based on animals with GABAergic neuronal dysfunctions
48. Effects of the nootropic drug nefiracetam on the GABAA receptor-channel complex in dorsal root ganglion neurons
49. Peripheral-type benzodiazepine receptors in association with epileptic seizures in EL mice
50. The benzodiazepine receptor in cultured astrocytes from genetically epilepsy-prone rats
51. Opposite effects of an agonist, RO5-4864, and an antagonist, PK 11195, of the peripheral type benzodiazepine binding sites on audiogenic seizures in DBA/2J mice
52. Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors
53. Nootropic nefiracetam inhibits proconvulsant action of peripheral-type benzodiazepines in epileptic mutant EL mice
54. Effects of DM-9384, a pyrrolidone derivative, on ischemia-induced changes in the central monoamine systems
55. Effects of nefiracetam (DM-9384), a pyrrolidone derivative, on brain monoamine systems
56. The effects of ritanserin, RU 24969 and 8-OH-DPAT on latent inhibition in the rat
57. Serotonergic mechanisms involved in the attentional and vigilance task performance of rats and the palliative action of aniracetam
58. Electrophysiological evidence for excitatory 5-HT2 and depressant 5-HT1A receptors on neurones of the rat midbrain tectum
59. Chronic exposure of rats to cognition enhancing drugs produces a neuroplastic response identical to that obtained by complex environment rearing
60. Environmental enrichment inhibits spontaneous apoptosis, prevents seizures and is neuroprotective
61. Influence of nefiracetam on NGF-induced neuritogenesis and neural cell adhesion molecule polysialic acid expression: in vivo and in vitro comparisons
62. Effects of N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide (DM-9384) on learning and memory in rats
63. Effects of nefiracetam on drug-induced impairment of latent learning in mice in a water finding task
64. Effects of DM-9384, a pyrrolidone derivative, on alcohol- and chlordiazepoxide-induced amnesia in mice
65. Nefiracetam (DM-9384) reverses apomorphine-induced amnesia of a passive avoidance response: delayed emergence of the memory retention effects
66. Involvement of the cholinergic system in the effects of nefiracetam (DM-9384) on carbon monoxide (CO)-induced acute and delayed amnesia
67. Nefiracetam (DM-9384) preserves hippocampal neural cell adhesion molecule-mediated memory consolidation processes during scopolamine disruption of passive avoidance training in the rat
68. Mecamylamine- or scopolamine-induced learning impairment: ameliorated by nefiracetam
69. Anticonvulsant and neuroprotective effects of the novel nootropic agent nefiracetam on kainic acid-induced seizures in rats
70. Anticonvulsant properties of the novel nootropic agent nefiracetam in seizure models of mice and rats
71. Effects of Nefiracetam, a novel pyrrolidone-type nootropic agent, on the amygdala-kindled seizures in rats
72. Improvement of depressive behaviors by nefiracetam is associated with activation of CaM kinases in olfactory bulbectomized mice
73. Double-blind treatment of apathy in patients with poststroke depression using nefiracetam
74. Double-blind randomized treatment of poststroke depression using nefiracetam
75. Syndromic validity of apathy in Alzheimer's disease
76. Reliability, validity, and clinical correlates of apathy in Parkinson's disease
77. Role of glutamate and glutamate receptors in memory function and Alzheimer's disease
78. Cholinesterase inhibitor therapy stabilizes symptoms of Alzheimer disease
79. Testicular toxicity induced in dogs by nefiracetam, a neutrotransmission enhancer
80. Single dose toxicity study of the new cognition-enhancing agent nefiracetam in mice, rats and dogs
81. Thirteen-week oral toxicity study of the new cognition-enhancing agent nefiracetam in dogs
82. Fifty-two-week oral toxicity study of the new cognition-enhancing agent nefiracetam in dogs
83. Examination of lesions in the urinary bladder and kidney of dogs induced by nefiracetam, a new nootropic agent
84. Investigation on urinary proteins and renal mRNA expression in canine renal papillary necrosis induced by nefiracetam
85. Early pathophysiological features in canine renal papillary necrosis induced by nefiracetam

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