RATIONALE The cannabinoid system consists of a complex array of receptors, substances with agonist/antagonist properties for those receptors, biosynthetic machineries and mechanisms for cellular uptake and degradation for endocannabinoids. This system is in interrelation with other systems that comprise lipid mediators like prostaglandins/leukotrienes systems. A clear antagonist, additive or sy...

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 ...

A physiological role for cannabinoids in the CNS is indicated by the presence of endogenous cannabinoids and cannabinoid receptors. However, the cellular mechanisms of cannabinoid actions in the CNS have yet to be fully defined. In the current study, we identified a novel action of cannabinoids to enhance intracellular Ca2+ responses in CNS neurons. Acute application of the cannabinoid receptor...

Introduction: It has been shown that administration of WIN55,212-2, a cannabinoid receptor agonist, into the basolateral amygdala (BLA), dose-dependently increases the thermal latency to withdrawal in the tail-.ick test and decreases pain related behaviors in both phases of the formalin test. Recent human and animal imaging data suggest that the nucleus accumbens (NAc) is an important neural su...

Introduction: Nucleus cuneiformis (NCF), as part of descending pain inhibitory system, cooperates with periaqueductal gray (PAG) and rostral ventromedial medulla (RVM) in supraspinal modulation of pain. Cannabinoids have analgesic effects in the PAG, RVM and NCF. The transient receptor potential vanilloid type 1(TRPV1) can be activated by anandamide and WIN55,212-2 as a cannabinoid receptor ago...

INTRODUCTION Ghrelin and cannabinoids stimulate appetite, this effect possibly being mediated by the activation of hypothalamic AMP-activated protein kinase (AMPK), a key enzyme in appetite and metabolism regulation. The cannabinoid receptor type 1 (CB1) antagonist rimonabant can block the orexigenic effect of ghrelin. In this study, we have elucidated the mechanism of the putative ghrelin-cann...

The receptors mediating the hemodynamic responses to cannabinoids are not clearly defined due to the multifarious pharmacology of many commonly used cannabinoid ligands. While both CB1 and TRPV1 receptors are implicated, G protein-coupled receptor 55 (GPR55) may also mediate some of the hemodynamic effects of several atypical cannabinoid ligands. The present studies attempted to unravel the pha...

Most of the cannabinoids in Cannabis sativa L. have not been fully evaluated for their pharmacological activity. A publication in this issue presents evidence that a plant cannabinoid, Delta(9)-tetrahydrocannabivarin is a potent antagonist of anandamide, a major endogenous cannabinoid. It seems possible that many of the non-psychoactive constituents of this plant will be of biological interest.

The present study was designed to explore the relationship between the cannabinoid and opioid receptors in animal models of opioid-induced reinforcement. The acute administration of SR141716A, a selective central cannabinoid CB1 receptor antagonist, blocked heroin self-administration in rats, as well as morphine-induced place preference and morphine self-administration in mice. Morphine-depende...