Cannabinoids regulate biological processes governed by the hypothalamus including, but not limited to, energy homeostasis and reproduction. The present study sought to determine whether cannabinoids modulate A-type K(+) currents (I(A)) in neurons of the hypothalamic arcuate nucleus (ARC). Whole cell patch-clamp recordings were performed in slices through the ARC prepared from castrated female a...

THE INTELLECTUAL INVENTION THAT SURPASSES ALL OTHERS AS THE MOST BENEFICIAL ADVANCE OF HUMAN HISTORY IS RARELY UNDERSTOOD OR APPRECIATED BY EDUCATED ADULTS. With dire consequences for such neglect, there has been no applause for this wondrous invention, no gratitude for its beneficence, no monuments to hail its priceless influence. Largely overlooked, ignored, or taken for granted, this unceleb...

A molecular docking approach was employed to evaluate the binding affinity of six triterpenes, namely epifriedelanol, friedelin, ?-amyrin, ?-amyrin acetate, ?-amyrin and bauerenyl towards cannabinoid type 1 receptor (CB1). Molecular studies showed that epifriedelanol had strongest CB1. dynamics simulation revealed friedelin engaged in stable non-bonding interactions by a pocket close active sit...

The human cannabinoid receptors, central cannabinoid receptor (CB1) and peripheral cannabinoid receptor (CB2), share only 44% amino acid identity overall, yet most ligands do not discriminate between receptor subtypes. Site-directed mutagenesis was employed as a means of mapping the ligand recognition site for the human CB2 cannabinoid receptor. A lysine residue in the third transmembrane domai...

Cannabinoids can activate CB1 and CB2 receptors. Since a CB2 mRNA has been described in rat peritoneal mast cells (RPMC), we investigated a series of cannabinoids and derivatives for their capacity to stimulate RPMC. Effects of natural cannabinoids v9-tetrahydrocannabinol (v9-THC), v8-THC, endocannabinoids (anandamide, palmitoylethanolamide) and related compounds (N-decanoyl-, N-lauroyl-, N-myr...

CB(1) cannabinoid receptor agonists show a different profile compared to other drugs of abuse on the basis of experimental data that reveal their reinforcing properties. Thus, there are controversial data in the literature concerning the ability of CB(1) receptor agonists to reinforce behavioral responses in experimental animals, i.e. to lower self-stimulation thresholds, and to support self-ad...

Extracts of Cannabis sativa have been used for their calming and sedative effects for centuries. Recent developments in drug discovery have suggested that modulation of neuronal endogenous cannabinoid signaling systems could represent a novel approach to the treatment of anxiety-related disorders while minimizing the adverse effects of direct acting cannabinoid receptor agonists. In this study,...