CB1 receptor

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The cannabinoid CB1 receptor is a G protein-coupled receptor (GPCR) that's found in high levels in the central nervous system (CNS). It's also found in the following areas of the brain: Neocortex, Hippocampus, Basal ganglia, Cerebellum, Brainstem.

The CB1 receptor regulates:

Neuronal transmission, Pain, Inflammation, Memory, Feeding behavior, Motor activity, Learning.

The CB1 receptor is activated by cannabinoids, which can be generated naturally or exogenously. Exogenous cannabinoids are usually found in cannabis or synthetic compounds.

Research suggests that:

• The majority of CB1 receptors are coupled through Gi/o proteins.
• Medium and high-intensity exercise can upregulate CB1 receptors and enhance their sensitivity.
• Within four weeks of stopping THC use, CB1 receptors should return to their original state.

Nabilone (Cesamet) is a synthetic analogue of THC that's been FDA approved as an antiemetic for chemotherapy patients. It's a CB1-R and CB2-R receptor agonist

A major limitation for the therapeutic development of compounds that directly activate CB1 receptors is unwanted psychotropic effects (Volkow et al., 2014). These CB1-mediated psychotropic actions produce both practical and administrative hurdles that have severely curtailed the development of direct-acting CB1 agonists.