ABSTRACT: The diversity of receptor signaling is increased by receptor heteromerization leading to dynamic regulation of receptor function. While a number of studies have demonstrated that family A G-protein-coupled receptors are capable of forming heteromers in vitro, the role of these heteromers in normal physiology and disease has been poorly explored. In this study, ... Continue Reading
cannabinoid receptors
STUDY: Analgesic effect of a mixed T-type channel inhibitor/CB2 receptor agonist
ABSTRACT: Cannabinoid receptors and T-type calcium channels are potential targets for treating pain. Here we report on the design, synthesis and analgesic properties of a new mixed cannabinoid/T-type channel ligand, NMP-181. Results NMP-181 action on CB1 and CB2 receptors was characterized in radioligand binding and in vitro GTPĪ³[35S] functional assays, and block of ... Continue Reading
STUDY: Inhibiting fatty acid amide hydrolase normalizes endotoxin-induced enhanced gastrointestinal motility in mice
ABSTRACT: BACKGROUND AND PURPOSE Gastrointestinal (GI) motility is regulated in part by fatty acid ethanolamides (FAEs), including the endocannabinoid (EC) anandamide (AEA). The actions of FAEs are terminated by fatty acid amide hydrolase (FAAH). We investigated the actions of the novel FAAH inhibitor AM3506 on normal and enhanced GI motility. EXPERIMENTAL ... Continue Reading
STUDY: The endocannabinoid system as a target for the treatment of motor dysfunction
ABSTRACT: There is evidence that cannabinoid-based medicines that are selective for different targets in the cannabinoid signalling system (e.g. receptors, inactivation mechanism, enzymes) might be beneficial in basal ganglia disorders, namely Parkinson's disease (PD) and Huntington's disease (HD). These benefits not only include the alleviation of specific motor symptoms ... Continue Reading
STUDY: Emerging Role of the CB2 Cannabinoid Receptor in Immune Regulation and Therapeutic Prospects
ABSTRACT: There is now a large body of data that indicates that the CB2 cannabinoid receptor type 2 (CB2) is linked to a variety of immune functional events. This functional relevance appears to be most salient in the course of inflammation, a process during which there is an increased number of receptors that are available for activation. Studies aimed at elucidating signal ... Continue Reading