Regionally selective and dose-dependent effects of the ampakines Org 26576 and Org 24448 on local cerebral glucose utilisation in the mouse as assessed by 14C-2-deoxyglucose autoradiography

@article{Jordan2005RegionallySA,  title={Regionally selective and dose-dependent effects of the ampakines Org 26576 and Org 24448 on local cerebral glucose utilisation in the mouse as assessed by 14C-2-deoxyglucose autoradiography},  author={Graeme R. Jordan and James Mcculloch and Mohammed Shahid and David R. Hill and Brian Henry and Karen Horsburgh},  journal={Neuropharmacology},  year={2005},  volume={49},  pages={254-264},  url={https://api.semanticscholar.org/CorpusID:24805124}}

27 Citations

Differential effects of AMPA receptor potentiators and glycine reuptake inhibitors on antipsychotic efficacy and prefrontal glutamatergic transmission

The results suggest that the AMPA-PAMs, when compared to the GlyT-1 inhibitor, show differential effects in terms of augmentation of antipsychotic efficacy, particularly when combined with risperidone or olanzapine.

Changes in AMPA subunit expression in the mouse brain after chronic treatment with the antidepressant maprotiline: a link between noradrenergic and glutamatergic function?

There could be an increase in calcium permeability of AMPA receptors in limbic/striatal brain regions after maprotiline treatment, which could lead to increased synaptic activity or plasticity in the hippocampus and striatum, and may underlie the therapeutic effect of maprotline, and possibly, other antidepressant drugs.

Preclinical Pharmacology of the Low-Impact Ampakine CX717

The pre-clinical pharmacology of ampakine 1-(benzofurazan-5-ylcarbonyl)morpholine (CX717) is described and support the continued clinical investigation of CX717 in the treatment of ADHD, dementia, and opiate-induced respiratory depression.

The ampakine, Org 26576, bolsters early spatial reference learning and retrieval in the Morris water maze: a subchronic, dose-ranging study in rats

Org 26576 offers early phase spatial memory benefits in rats, but particularly enhances search accuracy during reference memory retrieval, which supports its possible utility in treating disorders characterized by deficits in cognitive performance.

Chronic treatment with AMPA receptor potentiator Org 26576 increases neuronal cell proliferation and survival in adult rodent hippocampus

Findings suggest that Org 26576 may have antidepressant properties, which may be attributed, in part, to upregulation of hippocampal neurogenesis and prelimbic cell proliferation.

Positive Allosteric Modulation of Cholinergic Receptors Improves Spatial Learning after Cortical Contusion Injury in Mice

Benzyl quinolone carboxylic acid (BQCA) is a candidate compound to improve learning and memory function after brain trauma and may not suffer the associated central nervous system side effects typically associated with even modest doses of other cholinergic enhancers.

Translational PK–PD modelling of molecular target modulation for the AMPA receptor positive allosteric modulator Org 26576

A rat–human translational pharmacokinetic–pharmacodynamic (PK–PD) model of AMPA receptor modulation was used to predict human target engagement and inform dose selection in efficacy clinical trials and provided useful insight on the likely human dose–molecular target engagement relationship for Org 26576.

Therapeutic Potential of Positive AMPA Receptor Modulators in the Treatment of Neuropsychiatric Disorders

Animal studies characterising the pharmacological and behavioural effects of these substances have provided the rationale for several initial attempts to use these drugs in neuropsychiatric clinical settings, and applications in schizophrenia, Alzheimer’s disease and mild cognitive impairment have been initiated.

46 References

The AMPA Receptor Potentiator LY404187 Increases Cerebral Glucose Utilization and c-fos Expression in the Rat

These studies demonstrate neuronal activation in key brain areas that are associated with memory processes and thus provide an anatomical basis for the cognitive enhancing effects of AMPA receptor potentiators.

Positive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Modulators Have Different Impact on Synaptic Transmission in the Thalamus and Hippocampus

The regional selectivity of benzamide drugs (ampakines) may be explained by a lower potency at thalamic AMPA receptors, perhaps due to the prevalence of the subunits GluR3 and 4.

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