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CB1 Cannabinoid Receptors and On-Demand Defense Against Excitotoxicity
TLDR
The endogenous cannabinoid system provides on-demand protection against acute excitotoxicity in central nervous system neurons and could not be triggered in mutant mice.
Mitochondrial CB1 receptors regulate neuronal energy metabolism
TLDR
It is shown that the type-1 cannabinoid receptor (CB1) is present at the membranes of mouse neuronal mitochondria, where it directly controls cellular respiration and energy production, revealing a new mechanism of action of G protein–coupled receptor signaling in the brain.
Activation of the endocannabinoid system as a therapeutic approach in a murine model of multiple sclerosis
TLDR
The results indicate that treatment during established disease significantly improves the motor function of the diseased mice and suggest that agents able to activate the endocannabinoid system could constitute a new series of drugs for the treatment of MS.
The Antibacterial Cell Division Inhibitor PC190723 Is an FtsZ Polymer-stabilizing Agent That Induces Filament Assembly and Condensation*
TLDR
The biochemical action of PC190723 on FtsZ parallels that of the microtubule-stabilizing agent taxol on the eukaryotic structural homologue tubulin, and it is yet to be investigated whether both ligands target structurally related assembly switches.
Comparison of anandamide transport in FAAH wild-type and knockout neurons: evidence for contributions by both FAAH and the CB1 receptor to anandamide uptake.
TLDR
The results indicate that the protein-dependent uptake of AEA is largely mediated by known constituents of the endocannabinoid system (FAAH and the CB1 receptor), although a partial contribution of an additional UCM707-sensitive protein is also suggested.
A reversible and selective inhibitor of monoacylglycerol lipase ameliorates multiple sclerosis.
TLDR
A potent, selective, and reversible MAGL inhibitor is reported which is active in vivo and ameliorates the clinical progression of a multiple sclerosis mouse model without inducing undesirable CB1 -mediated side effects and support the interest in MAGL as a target for the treatment of MS.
The Role of Internal Water Molecules in the Structure and Function of the Rhodopsin Family of G Protein‐Coupled Receptors
TLDR
The availability of the rhodopsin structure allows the use of homology modeling techniques to build three-dimensional models of other homologous GPCRs, and a large number of conserved sequence patterns suggest a common TM structure.
Design, synthesis and biological evaluation of new endocannabinoid transporter inhibitors.
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
TLDR
It is hoped that these compounds, particularly the most potent in this series (compound 5, UCM707, with IC(50) values for anandamide uptake and FAAH of 0.8 and 30 microM, respectively), will provide useful tools for the elucidation of the role of the an andamide transporter system in vivo.
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