GPR18, GPR55 and GPR119 (provisional nomenclature), although showing little structural similarity to CB1 CB2 cannabinoid receptors, respond endogenous agents analogous the ligands, as well some natural/synthetic receptor ligands [104]. Although there are multiple reports indicate that can be activated in vitro by N-arachidonoylglycine, lysophosphatidylinositol N-oleoylethanolamide, respectively...

The plant Cannabis has been known for centuries to be beneficial in a variety of gastrointestinal diseases, including emesis, diarrhea, inflammatory bowel disease and intestinal pain. delta9-tetrahydrocannabinol, the main psychotropic component of Cannabis, acts via at least two types of cannabinoid receptors, named CB1 and CB2 receptors. CB1 receptors are located primarily on central and perip...

Type-1 cannabinoid (CB1) and leptin (ObR) receptors regulate metabolic and astroglial functions, but the potential links between the two systems in astrocytes were not investigated so far. Genetic and pharmacological manipulations of CB1 receptor expression and activity in cultured cortical and hypothalamic astrocytes demonstrated that cannabinoid signaling controls the levels of ObR expression...

INTRODUCTION The endocannabinoid system is composed of endogenous ligands, their enzymes for biosynthesis and degradation and cannabinoid receptors (13). The CB1 receptor is one of the most abundant G protein-coupled receptors expressed in the central nervous system (5). The regional distribution of CB1 receptors has been described in the rat brain (10, 15). During aging the number of CB1 recep...

Cannabinoids exert various biological effects that are either receptor-mediated or independent of receptor signaling. Mitochondrial effects of cannabinoids were interpreted either as non-receptor-mediated alteration of mitochondrial membranes, or as indirect consequences of activation of plasma membrane type 1 cannabinoid receptors (CB1). Recently, CB1 receptors were confirmed to be localized t...

Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds (I-IV) along with eleven known compounds (V-XV). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (-49.7 and -53.8% displacement, resp.). Compound ...

The pharmacology of 3-(2-ethylmorpholino)-5,5'-di(p-bromophenyl)-imidazolidinedione (DML20), 3-(1-hydroxypropyl)-5,5'-di(p-bromophenyl)-imidazolidinedione (DML21) and 3-heptyl-5,5'-di(p-bromophenyl)-imidazolidinedione (DML23) was extended by studying affinity and GTP binding modulation on cannabinoid receptor subtypes (CB1 and CB2) from rat tissues and human cannabinoid receptors expressed in C...

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...

Dopamine and endogenous cannabinoids display complex interactions in the basal ganglia. One possible level of interaction is between CB1 cannabinoid and D2 dopamine receptors. Here, we demonstrate that a regulated association of CB1 and D2 receptors profoundly alters CB1 signaling. This provides the first evidence that CB1/D2 receptor complexes exist, are dynamic, and are agonist-regulated with...

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...