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Identification and Functional Characterization of Brainstem Cannabinoid CB2 Receptors
TLDR
These functional CB2 receptors in the brainstem were activated by a CB2 receptor agonist, 2-arachidonoylglycerol, and by elevated endogenous levels of endocannabinoids, which also act at CB1 receptors.
Functional role of high-affinity anandamide transport, as revealed by selective inhibition.
TLDR
The data indicate that carrier-mediated transport may be essential for termination of the biological effects of anandamide, and may represent a potential drug target.
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
TLDR
The iodinated nature of this compound offers additional utility as a gamma-enriching SPECT (single photon emission computed tomography) ligand that may be useful in characterizing brain CB1 receptor binding in vivo.
Endocannabinoids control spasticity in a multiple sclerosis model
TLDR
These studies provide definitive evidence for the tonic control of spasticity by the endocannabinoid system and open new horizons to therapy of multiple sclerosis, and other neuromuscular diseases, based on agents modulating endoc cannabinoidoid levels and action, which exhibit little psychotropic activity.
Anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor AM1172.
TLDR
The results indicate that anandamideinternalization in mouse brain neurons is independent of FAAH activity, and the compound N-(5Z, 8Z, 11Z, 14Z eicosatetraenyl)-4-hydroxybenzamide (AM1172) blocked [(3)H]anandamide internalization in rodent cortical neurons and human astrocytoma cells without acting as a FAAH substrate or inhibitor.
(R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability.
TLDR
Determination of the cannabinoid binding affinity in the presence and absence of the protease inhibitor phenylmethanesulfonyl fluoride (PMSF) revealed that (R)-methanandamide possesses a remarkable stability to aminopeptidase hydrolysis, and experiments with mice have demonstrated that it possesses cannabimimetric properties in vivo.
Convergent translational evidence of a role for anandamide in amygdala-mediated fear extinction, threat processing and stress-reactivity
TLDR
The findings show that augmenting amygdala anandamide enables extinction-driven reductions in fear in mouse and may promote stress-coping in humans.
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