Neuroscience Research Compound · For laboratory research use only
Also known as ISF-2522
Oxiracetam (2-(4-hydroxy-2-oxopyrrolidin-1-yl)acetamide) is a member of the racetam family that carries a hydroxyl group at the 4-position of the pyrrolidinone ring found in piracetam. It is a racemic compound; a 2017 rat study identified the (S)-enantiomer as the active ingredient in a chronic cerebral hypoperfusion model5.
Preclinical studies have examined hippocampal neurotransmission in rat brain slices, cholinergic and learning models in rats and mice, cerebral hypoperfusion in rats and microglial inflammation in vitro1,2,3,4,5,6. A multicentre clinical trial in post-stroke cognitive impairment has published its design7.
As described in the research literature
As described in the research literature, superfusion of rat hippocampal slices with oxiracetam produced a concentration-dependent, wash-resistant increase in the field excitatory postsynaptic potential in the CA1 region. The effect shared features with long-term potentiation: it persisted, was blocked by the NMDA receptor antagonist AP-5 and did not add to electrically induced potentiation1.
In superfused rat hippocampal slices, low concentrations increased potassium-evoked release of [3H]D-aspartate and, less effectively, [3H]acetylcholine, without affecting GABA, noradrenaline or serotonin release; the effect was not seen in synaptosomes, suggesting a site of action outside the releasing nerve terminals2. In learning-impaired DBA/2 mice, spatial learning measures correlated with an increase in membrane-bound protein kinase C in the hippocampus4.
What published studies have examined
Extracellular recordings in the CA1 region of rat hippocampal slices examined field potentials, input-output relationships and interaction with long-term potentiation1. Release of radiolabelled glutamate analogue, acetylcholine, GABA, noradrenaline and serotonin was compared in hippocampal slices and synaptosomes2.
Overtrained rats in a radial arm maze were used to examine disruption of performance by scopolamine and its interaction with oxiracetam, compared with physostigmine and methylscopolamine3. C57BL/6 and DBA/2 mice were compared on the Morris water maze and contextual fear conditioning, with hippocampal protein kinase C activity measured in subcellular fractions4.
In rats with chronic cerebral hypoperfusion, (S)- and (R)-oxiracetam were compared for spatial learning, neuronal damage, white matter lesions, cerebral blood flow and astrocyte activation, with MALDI mass spectrometry imaging and LC-MS/MS used to examine ATP metabolism, glutamine-glutamate and antioxidants in cortex5.
Sources [5]
BV2 microglial cells stimulated with amyloid-beta 42 oligomers were used to examine morphology, phagocytosis, IL-1beta, IL-6, TNF-alpha and nitric oxide production, and conditioned medium was applied to HT22 hippocampal cells to assess indirect toxicity6.
Sources [6]
A multicentre, randomised, double-blind, placebo-controlled phase IV trial in patients with cognitive decline after stroke (registration KCT0005137) was designed with co-primary endpoints of change in the Mini-Mental State Examination and the Clinical Dementia Rating Sum of Boxes, and included an exercise protocol with actigraphy to examine interaction with physical activity7.
Sources [7]
Effect of the nootropic drug oxiracetam on field potentials of rat hippocampal slices.
Pugliese AM, Corradetti R, Ballerini L, et al. British Journal of Pharmacology, 1990.
Effects of oxiracetam on neurotransmitter release from rat hippocampus slices and synaptosomes.
Raiteri M, Costa R, Marchi M Neuroscience Letters, 1992.
Oxiracetam antagonizes the disruptive effects of scopolamine on memory in the radial maze.
Magnani M, Pozzi O, Biagetti R, et al. Psychopharmacology, 1992.
Enhancement of hippocampally-mediated learning and protein kinase C activity by oxiracetam in learning-impaired DBA/2 mice.
Fordyce DE, Clark VJ, Paylor R, et al. Brain Research, 1995.
(S)-Oxiracetam is the Active Ingredient in Oxiracetam that Alleviates the Cognitive Impairment Induced by Chronic Cerebral Hypoperfusion in Rats.
Li W, Liu H, Jiang H, et al. Scientific Reports, 2017.
Oxiracetam Offers Neuroprotection by Reducing Amyloid β-Induced Microglial Activation and Inflammation in Alzheimer's Disease.
Zhang H, Jia L, Jia J Frontiers in Neurology, 2020.
Efficacy and safety of oxiracetam in patients with vascular cognitive impairment: A multicenter, randomized, double-blinded, placebo-controlled, phase IV clinical trial.
Lim JS, Lee J, Kang Y, et al. Contemporary Clinical Trials, 2023.
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