Recent developments have implicated cannabinoid CB1 receptors as a novel target for a new class of therapeutic agents used to treat drug addiction. CB1 receptors are expressed in the motivational circuitry of the brain and modulate drug seeking. Blockade of the CB1 receptor is particularly effective in reducing cue-induced reinstatement of drug seeking, an animal analogue of cue-induced relapse...

Metabolic syndrome (MS) is a known risk factor for lower urinary tract symptoms. This study investigates whether functional and expression changes of cannabinoid CB1 and CB2 receptors are involved in the bladder dysfunction in an obese rat model with insulin resistance. Bladder samples from obese Zucker rat (OZR) and their respective controls lean Zucker rat (LZR) were processed for immunohisto...

The recent identification and cloning of guanine nucleotide regulatory protein-coupled brain-type and spleen-type cannabinoid receptors (CB1-R and CB2-R, respectively) provide evidence that many of the effects of cannabinoids are mediated via these receptors. Our recent observation of expression of both CB1-R and CB2-R genes in the preimplantation mouse embryo suggests that it could also be a t...

Although endocannabinoid signaling is important for certain aspects of gastrointestinal homeostasis, the role of the cannabinoid receptors (CB) in colorectal cancer has not been defined. Here we show that CB1 expression was silenced in human colorectal cancer due to methylation of the CB1 promoter. Our genetic and pharmacologic studies reveal that loss or inhibition of CB1 accelerated intestina...

endocannabinoid (ecb) system plays a vital role in responses to stress. moreover, ecb and its receptors cause anti-inflammatory, anti-oxidative and neuroprotective effects by modulating neuronal, glial and endothelial cell functions. a number of studies have demonstrated ecb system notably defects in neurotraumatic and neurodegenerative diseases like epilepsy, tbi, alzheimer’s disease and parki...

AM 251 ALX-270-239-M001 1 mg ALX-270-239-M005 5 mg Structurally related to the cannabinoid receptor (CB) antagonist SR 141716A. Binds with high affinity to cannabinoid receptor CB1 (Ki=7.49nM; 306-fold selective over CB2 receptors). LIT: Binding of the non-classical cannabinoid CP 55, 940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors: S.J. Gatley, et al.; Life Sci. 61, PL ...

Introduction: Previous studies have shown that cannabinoidergic system is involved in anxiety. However, there are controversial reports in the experimental studies. The aim of this study is to evaluate the effect of pharmacological stimulation or blocking of CB1 receptors and inhibition of endocannabinoid degradation in anxiety like behavior in elevated plus-maze (EPM) test in rat. The EPM is o...

CB1 and CB2 cannabinoid receptors are the primary targets of endogenous cannabinoids (endocannabinoids). These G protein-coupled receptors play an important role in many processes, including metabolic regulation, craving, pain, anxiety, bone growth, and immune function. Cannabinoid receptors can be engaged directly by agonists or antagonists, or indirectly by manipulating endocannabinoid metabo...

objective (s):hyperglycemia is widely recognized as the underlying cause for some debilitating conditions in diabetic patients. the role of cannabinoid cb1 and vanilloid trpv1 receptors and their endogenous agonists, endovanilloids, in diabetic neuropathy is shown in many studies. here we have used pc12 cell line to investigate the possible influence of glucose concentration in culture medium o...

Cannabinoids affect diverse biological processes, including functions of the immune system. With respect to the immune system, anti-inflammatory and immunosuppressive effects of cannabinoids have been reported. Cannabinoids stimulate G protein-coupled cannabinoid receptors CB1 and CB2. These receptors are found primarily on neurons. However, they are also found on dendritic cells (DC), which ar...