CB1 cannabinoid receptor agonists induce acute respiratory depression in awake mice☆
Abstract Recreational use of synthetic cannabinoid agonists (i.e., “spice compounds”) that target the cannabinoid type 1 receptor (CB1) can cause…
Alexandros Makriyannis
Structural basis of THC analog activity at the Cannabinoid 1 receptor
Abstract Tetrahydrocannabinol (THC) is the principal psychoactive compound derived from the cannabis plant Cannabis sativa and approved for emetic conditions,…
Comparison of Agonist Activity between CB1 and CB2 Receptors with Orthosteric Site Mutations
Abstract Human endocannabinoid signaling is primarily mediated by the cannabinoid receptors, CB1 and CB2, which are G protein-coupled receptors (GPCRs).…
Cannabinoids Block Fat-induced Incretin Release via CB1-dependent and CB1-independent Pathways in Intestinal Epithelium
Abstract Background and Aims: Glucose homeostasis is regulated by a dynamic interplay between hormones along the gastro-insular axis. For example,…
Structural basis of Δ9-THC analog activity at the Cannabinoid 1 receptor
Abstract Δ9-tetrahydrocannabinol (THC) is the principal psychoactive compound derived from the cannabis plant Cannabis sativa and approved for emetic conditions,…
Structural basis for activation of CB1 by an endocannabinoid analog
Abstract Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a G protein-coupled receptor that regulates a number…
Effects of cannabinoid exposure on short-term memory and medial orbitofrontal cortex function and chemistry in adolescent female rhesus macaques
Abstract Aim: There is increasing concern that cannabinoid exposure during adolescence may disturb brain maturation and produce long-term cognitive deficits.…
Reversal of diet-induced hepatic steatosis by peripheral CB1 receptor blockade in mice is p53/miRNA-22/SIRT1/PPARα dependent
Abstract Objective: The endocannabinoid (eCB) system is increasingly recognized as being crucially important in obesity-related hepatic steatosis. By activating the…
Synthesis of Functionalized Cannabilactones
Abstract A new approach to synthesize cannabilactones using Suzuki cross-coupling reaction followed by one-step demethylation-cyclization is presented. The two key…
Controlled-Deactivation CB1 Receptor Ligands as a Novel Strategy to Lower Intraocular Pressure
Abstract Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ9-THC lowers intraocular…