Equipotent Inhibition of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase – Dual Targets of the Endocannabinoid System to Protect against Seizure Pathology

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Neurotherapeutics

• Publication date

  2012-01-20

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1007/s13311-011-0100-yPMID 22270809PMCID PMC3480564
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Endocannabinoid 2-arachidonoylglycerol protects neurons against β-amyloid insults.

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  2011influential reference
• Effects of Endocannabinoid System Modulation on Cognitive and Emotional Behavior

  2011cited by this paper
• Homeostatic changes of the endocannabinoid system in Parkinson's disease

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• Cannabinoid receptor activation modifies NMDA receptor mediated release of intracellular calcium: implications for endocannabinoid control of hippocampal neural plasticity.

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• Dual-target-directed drugs that block monoamine oxidase B and adenosine A2A receptors for Parkinson’s disease

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• Differential role of anandamide and 2-arachidonoylglycerol in memory and anxiety-like responses.

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• Worsening of Huntington disease phenotype in CB1 receptor knockout mice.

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• Hippocampal expression and distribution of CB1 receptors in the Amazonian rodent Proechimys: an animal model of resistance to epilepsy.

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• Enhancement of endocannabinoid signaling by fatty acid amide hydrolase inhibition: a neuroprotective therapeutic modality.

  2010cited by this paper
• Cannabinoid receptors in brain: pharmacogenetics, neuropharmacology, neurotoxicology, and potential therapeutic applications.

  2009cited by this paper
• Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo

  2009cited by this paper
• Pharmacotherapeutic modulation of the endocannabinoid signalling system in psychiatric disorders: Drug-discovery strategies

  2009cited by this paper
• BDNF mediates the neuroprotective effects of positive AMPA receptor modulators against MPP+-induced toxicity in cultured hippocampal and mesencephalic slices.

  2009cited by this paper
• Refined homology model of monoacylglycerol lipase: toward a selective inhibitor

  2009cited by this paper
• Covalent inhibitors of human monoacylglycerol lipase: ligand-assisted characterization of the catalytic site by mass spectrometry and mutational analysis.

  2008cited by this paper
• Endocannabinoids: synthesis and degradation.

  2008cited by this paper
• Inhibition of endocannabinoid metabolism attenuates enhanced hippocampal neuronal activity induced by kainic acid

  2008cited by this paper
• Calpain activation is involved in early caspase‐independent neurodegeneration in the hippocampus following status epilepticus

  2008cited by this paper
• Gephyrin Alterations Due to Protein Accumulation Stress are Reduced by the Lysosomal Modulator Z-Phe-Ala-Diazomethylketone

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• Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation.

  2008cited by this paper
• Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.

  2008cited by this paper
• Enzymatic pathways that regulate endocannabinoid signaling in the nervous system.

  2008cited by this paper
• Endocannabinoids and cannabinoid receptors in ischaemia–reperfusion injury and preconditioning

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• Downregulation of the CB1 Cannabinoid Receptor and Related Molecular Elements of the Endocannabinoid System in Epileptic Human Hippocampus

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• Endocannabinoid Enhancement Protects against Kainic Acid-Induced Seizures and Associated Brain Damage

  2007influential reference
• Truncations of amphiphysin I by calpain inhibit vesicle endocytosis during neural hyperexcitation

  2007cited by this paper
• Critical enzymes involved in endocannabinoid metabolism.

  2007cited by this paper
• The complications of promiscuity: endocannabinoid action and metabolism

  2007cited by this paper
• The Multiple Pathways of Endocannabinoid Metabolism: A Zoom Out

  2007cited by this paper
• Endocannabinoids and neurodegenerative diseases.

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• Targeting the endocannabinoid system in treating brain disorders

  2006cited by this paper
• Extrasynaptic Membrane Trafficking Regulated by GluR1 Serine 845 Phosphorylation Primes AMPA Receptors for Long-term Potentiation*

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• Preparation of organotypic hippocampal slice cultures for long-term live imaging

  2006cited by this paper
• Effects of switching from an AChE inhibitor to a dual AChE-BuChE inhibitor in patients with Alzheimer's disease.

  2005cited by this paper
• Dual Modulation of Endocannabinoid Transport and Fatty Acid Amide Hydrolase Protects against Excitotoxicity

  2005influential reference
• Mechanism of carbamate inactivation of FAAH: implications for the design of covalent inhibitors and in vivo functional probes for enzymes.

  2005cited by this paper
• Neuroprotective effects of the synthetic cannabinoid HU-210 in primary cortical neurons are mediated by phosphatidylinositol 3-kinase/AKT signaling.

  2005cited by this paper
• A fluorescence-based assay for fatty acid amide hydrolase compatible with high-throughput screening.

  2005cited by this paper
• Empirical evidence of neuroprotection by dual cholinesterase inhibition in Alzheimer's disease

  2005cited by this paper
• Effects of switching from an AChE inhibitor to a dual AChE-BuChE inhibitor in patients with Alzheimer's disease

  2005cited by this paper
• Segregation of two endocannabinoid‐hydrolyzing enzymes into pre‐ and postsynaptic compartments in the rat hippocampus, cerebellum and amygdala

  2004cited by this paper
• Biphasic NF-κB activation in the excitotoxic hippocampus

  2004cited by this paper
• Biphasic NF-kappaB activation in the excitotoxic hippocampus.

  2004cited by this paper
• Comparative analysis of fatty acid amide hydrolase and cb(1) cannabinoid receptor expression in the mouse brain: evidence of a widespread role for fatty acid amide hydrolase in regulation of endocannabinoid signaling.

  2003cited by this paper
• Combination drug therapy and mild hypothermia after transient focal cerebral ischemia in rats.

  2003cited by this paper
• Phosphorylation of the AMPA receptor GluR1 subunit is required for synaptic plasticity and retention of spatial memory.

  2003cited by this paper
• Cannabinoid CB2 Receptors and Fatty Acid Amide Hydrolase Are Selectively Overexpressed in Neuritic Plaque-Associated Glia in Alzheimer's Disease Brains

  2003cited by this paper
• AMPA receptors regulate dynamic equilibrium of presynaptic terminals in mature hippocampal networks

  2003cited by this paper
• CB1 Cannabinoid Receptors and On-Demand Defense Against Excitotoxicity

  2003cited by this paper
• Levodopa treatment reverses endocannabinoid system abnormalities in experimental parkinsonism

  2003cited by this paper
• Brain monoglyceride lipase participating in endocannabinoid inactivation

  2002cited by this paper
• Advances in the Treatment of Alzheimer’s Disease: Benefits of Dual Cholinesterase Inhibition

  2002cited by this paper
• Mechanism of extracellular signal-regulated kinase activation by the CB(1) cannabinoid receptor.

  2002cited by this paper
• Survival signaling and selective neuroprotection through glutamatergic transmission.

  2002cited by this paper
• Increased Severity of Stroke in CB1 Cannabinoid Receptor Knock-Out Mice

  2002cited by this paper
• Anandamide, but not 2‐arachidonoylglycerol, accumulates during in vivo neurodegeneration

  2001cited by this paper
• Kainic acid-induced dorsal and ventral hippocampal seizures in rats.

  2001cited by this paper
• Endogenous cannabinoids mediate retrograde signals from depolarized postsynaptic neurons to presynaptic terminals.

  2001cited by this paper
• Presynaptic specificity of endocannabinoid signaling in the hippocampus.

  2001cited by this paper
• Retrograde inhibition of presynaptic calcium influx by endogenous cannabinoids at excitatory synapses onto Purkinje cells.

  2001cited by this paper
• Accessory factors in clathrin-dependent synaptic vesicle endocytosis

  2000cited by this paper
• Cannabinoids inhibit hippocampal GABAergic transmission and network oscillations

  2000cited by this paper
• Reinsertion or degradation of AMPA receptors determined by activity-dependent endocytic sorting.

  2000cited by this paper
• Control of GluR1 AMPA Receptor Function by cAMP-Dependent Protein Kinase

  2000cited by this paper
• The pathogenic activation of calpain: a marker and mediator of cellular toxicity and disease states

  2000cited by this paper
• The CB1 cannabinoid receptor is coupled to the activation of protein kinase B/Akt.

  2000cited by this paper
• Combination drug therapy and mild hypothermia: a promising treatment strategy for reversible, focal cerebral ischemia.

  1999cited by this paper
• Functional partnership between amphiphysin and dynamin in clathrin-mediated endocytosis

  1999cited by this paper
• A new perspective on cannabinoid signalling: complimentary localization of fatty acid amide hydrolase and the CB1 receptor in rat brain.

  1998cited by this paper
• Comparative characterization of a wild type and transmembrane domain-deleted fatty acid amide hydrolase: identification of the transmembrane domain as a site for oligomerization.

  1998cited by this paper
• A role of amphiphysin in synaptic vesicle endocytosis suggested by its binding to dynamin in nerve terminals.

  1996cited by this paper
• Long‐term hippocampal slices: A model system for investigating synaptic mechanisms and pathologic processes

  1995cited by this paper
• Cannabinoids modulate voltage sensitive potassium A-current in hippocampal neurons via a cAMP-dependent process.

  1995cited by this paper
• Induction of calpain-mediated spectrin fragments by pathogenic treatments in long-term hippocampal slices.

  1995cited by this paper

• Endocannabinoid signaling in epilepsy.

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