ABSTRACT: Historically and anecdotally cannabinoids have been used as analgesic agents. In recent years, there has been an escalating interest in developing cannabis-derived medications to treat severe pain. This review provides an overview of the history of cannabis use in medicine, cannabinoid signaling pathways, and current data from preclinical as well as clinical ... Continue Reading
Pain
STUDY: Inhibition of human recombinant T-type calcium channels by the endocannabinoid N-arachidonoyl dopamine
ABSTRACT: Background and purpose: N-arachidonoyl dopamine (NADA) has complex effects on nociception mediated via cannabinoid CB1 receptors and the transient receptor potential vanilloid receptor 1 (TRPV1). Anandamide, the prototypic CB1/TRPV1 agonist, also inhibits T-type voltage-gated calcium channel currents (ICa). These channels are expressed by many excitable cells, ... Continue Reading
STUDY: Modulating the endocannabinoid system in human health and disease: successes and failures
ABSTRACT: The discovery of the endocannabinoid system (ECS; comprising of G-protein coupled cannabinoid 1 and 2 receptors, their endogenous lipid ligands or endocannabinoids, and synthetic and metabolizing enzymes, triggered an avalanche of experimental studies that have implicated the ECS in a growing number of physiological/pathological functions. They also suggested that ... Continue Reading
STUDY: N-Acyl amino acids and N-acyl neurotransmitter conjugates: neuromodulators and probes for new drug targets
ABSTRACT: The myriad functions of lipids as signalling molecules is one of the most interesting fields in contemporary pharmacology, with a host of compounds recognized as mediators of communication within and between cells. The N-acyl conjugates of amino acids and neurotransmitters (NAANs) have recently come to prominence because of their potential roles in the nervous ... Continue Reading
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 GTPγ[35S] functional assays, and block of ... Continue Reading