Cannabinoid receptor 1 and endocannabinoid transport system (CB1/EMT)

Cannabinoid receptor 1 (CB1) is a G protein-coupled receptor predominantly expressed in the central nervous system, where it modulates the release of various neurotransmitters including GABA and glutamate (UniProt: P21554). The endocannabinoid transport system encompasses the mechanisms responsible for the cellular uptake of endogenous ligands like anandamide, which is a crucial step in terminating their biological signaling (PubMed: 23501877). This combined system plays a pivotal role in regulating appetite, pain sensation, mood, and memory. Dysregulation of CB1 and endocannabinoid transport is linked to obesity, chronic pain, and neurodegenerative diseases (StatPearls: NBK542221). Therapeutic strategies include CB1 agonists for pain and nausea, and transport inhibitors to enhance natural endocannabinoid levels. However, clinical use of CB1 antagonists has been limited by severe psychiatric side effects, such as depression and suicidal ideation (PubMed: 18445618).

Other names

CB1RCNR1Anandamide transporterEndocannabinoid membrane transporterCannabinoid receptor 1 / endocannabinoid transporter systems

Drugs targeting this system act as agonists or antagonists at the Cannabinoid receptor 1 to modulate intracellular signaling, or as inhibitors of the endocannabinoid transport system to prevent the reuptake and degradation of endogenous ligands like anandamide, thereby prolonging their physiological effects (PubMed: 23501877, StatPearls: NBK542221).