The involvement of endocannabinoid receptors in the antinociceptive activity Lonchocarpus araripensis lectin (LAL) was investigated model carragenan-induced hypernociception. Swiss mice received LAL (10 mg/kg) by intravenous (i.v.) route 30 min before subcutaneous (s.c.) injection carrageenan paws. Animals were treated with antagonists CB1 (AM251) or CB2 (AM630) cannabinoid lectin. inhibited hy...

Transient global cerebral ischemia (TGCI) induces by bilateral common carotid artery occlusion (BCCAO), and it mediates neuronal cell death of the CA1 hippocampal area. AM251 is a cannabinoid receptors type 1 (CB1) blocker that has been known to be protective against transient focal cerebral ischemia. JWH-015 is a selective agonist of CB2 and activator of CB1 that is involved in promotion of ne...

Blockade of cannabinoid CB1 receptors has been reported to inhibit cocaine- or cocaine cue-induced reinstatement of drug seeking. However, the mechanisms underlying this action are poorly understood. Given the importance of dopamine, glutamate, and GABA in cocaine reward and relapse, we studied the effects of AM251 [N-(piperidin-1-yl)-5-(4-iodophonyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole...

In the last few years, an increasing interest in neuroprotective effect of cannabinoids has taken place. The aim present work was to study effects modulating cannabinoid receptor 1 (CB1) context light induced retinal degeneration (LIRD), using animal model that resembles many characteristics human age-related macular (AMD) and other degenerative diseases outer retina. Sprague Dawley rats ( n = ...

conclusions ip injection of cb1 receptor antagonist might have an anxiogenic profile in rat, whereas calcium channel blocker attenuated the anxiogenic effect of am251. our results suggest that there is an interaction between functions of l-type ca2+ channels and cannabinoid system in anxiety. background the elevated plus-maze (epm) has been broadly used to investigate anxiolytic and anxiogenic ...

High density of cannabinoid receptors type 1 (CB1) in the brain suggests that endocannabinoid system plays an important role in the functioning of the central nervous system. Natural and synthetic cannabinoids are known to attenuate learning and memory processes. The adverse effects of cannabinoids are reversed by SR141716A, at first reported to be a selective CB1 receptor antagonist, later sho...

Modulation of the endocannabinoid system as an anti-obesity therapeutic is well established; however, the direct effects of cannabinoid receptor 1 (CB1) antagonism on renal function and structure in a model of diet-induced obesity (DIO) are unknown. The aim of this study was to characterise the renal effects of the CB1 antagonist AM251 in a model of DIO. Male Sprague-Dawley rats were fed a low-...

Epithelial-mesenchymal transition (EMT) of renal tubular epithelial cells is one of the causative mechanisms of kidney fibrosis. In our study, we screened lipophilic compounds using a lipid library including approximately 200 lipids to identify those that suppressed EMT induced by a transforming growth factor (TGF)-β1 stimulus. Initial screening was performed with the immortalized HK-2 renal tu...

The effects of CB1 antagonist/inverse agonists on the acquisition and consolidation of conditioned fear remain uncertain. Recent studies suggest that the CB1 antagonist/inverse agonist AM251 affects acquisition or consolidation of both contextual and discretely cued fear memories. AM251 is frequently referred to as a CB1 antagonist; however in vitro signal transduction assays indicate that this...

Under adverse environmental conditions the nematode Caenorhabditis elegans can enter an alternate developmental stage called the dauer larva. To identify lipophilic signaling molecules that influence this process, we screened a library of bioactive lipids and found that AM251, an antagonist of the human cannabinoid (CB) receptor, suppresses dauer entry in daf-2 insulin receptor mutants. AM251 a...