
Inversago Pharma - Model CB1 - The Endocannabinoid System
CB1 Receptors: Signaling the Brain from the Periphery: The endocannabinoid system is responsible for both homeostasis and equilibrium of the human metabolism. It is involved in regulating several pathways linked to energy intake, reserves and overall expenditure. To do so, the cannabinoid-1 receptor (CB1) may be activated and deactivated such that it impacts many metabolic pathways involving several enzymes and proteins, e.g. leptin, insulin and ghrelin.
While the highest density of CB1 receptors are located in the brain, most cells outside of the central nervous system (hepatocytes, β-cells, adipocytes, myocytes, epithelial cells of the GI tract, etc.) also express the CB1 receptor.
The peripheral endocannabinoid system is now recognized as an important driver in the multi-indication efficacy observed with first generation CB1 antagonists like rimonabant. As such, a safe and potent CB1 inhibitor has the potential to block or reverse (inverse agonize) the biological processes induced by their activation and treat several metabolic indications.