We tested the hypothesis that human CB1 cannabinoid receptors (hCB1) can sequester G(i/o)-proteins from a common pool and prevent other receptors from signaling. Human CB1 cannabinoid receptors were expressed in superior cervical ganglion (SCG) neurons by microinjection of hCB1 cDNA. Expression of hCB1 cannabinoid receptors abolished the Ca(2+) current inhibition by endogenous pertussis toxin-s...

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 ...

BACKGROUND Systemic administration of cannabinoid agonists is known to reduce pain induced by bladder inflammation and to modulate cystometric parameters in vivo. We have previously reported that intravesical administration of a cannabinoid agonist reduces the electrical activity of bladder afferents under normal conditions. However, the effects of local activation of bladder cannabinoid recept...

The effect of anandamide, an endogenous ligand for central (CB1) and peripheral (CB2) cannabinoid receptors, was investigated on the growth of the murine IL-6-dependent lymphoid cell line B9 and the murine IL-3-dependent myeloblastic cell line FDC-P1. In conditions of low serum level, anandamide potentiated the growth of both cytokine-dependent cell lines. Comparison with other fatty acid canna...

anandamide is an endogenous ligand for cannabinoid receptors and has endothelial protective effect against ischemic preconditioning. the purpose of this study was to investigate the effects of cannabinoids on reperfusion injury due to testicular torsion-detorsion (t/d). a total of 36 adult male sprague-dawley rats were divided into 6 groups. testicular ischemia was achieved by twisting the righ...

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...

The human body possesses specific binding sites on the surface of many cell types for cannabinoids, and our body produces several endocannabinoids, fatty acid derivatives that bind to these cannabinoid receptors (CB) and activate them. CB receptors and endocannabinoids together constitute the endocannabinoid system. Some phytocannabinoids, cannabinoids of the cannabis plant, and a multitude of ...

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...

Cannabinoid pharmacology has made important advances in recent years after the cannabinoid system was discovered. Studies in experimental models and in humans have produced promising results using cannabinoid-based drugs for the treatment of obesity and cancer, as well as neuroinflammatory and chronic inflammatory diseases. Moreover, as we discuss here, additional studies also indicates that th...

Cannabinoids, as multi‑target mediators, activate cannabinoid receptors and transient receptor potential vanilloid (TRPV) channels. There is evidence to support a functional interaction of cannabinoid receptors and TRPV channels when they are coexpressed. Human conjunctiva demonstrates widespread cannabinoid receptor type 1 (CB1), CB2 and TRPV channel localization. The aim of the present study ...