Cannabinoid receptor 1

Cannabinoid receptor 1 (CB1) is a G protein-coupled receptor that in humans is encoded by the CNR1 gene. The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. It is activated by cannabinoids, a group of compounds that include the active components of cannabis (marijuana), and by the endogenous cannabinoids anandamide and 2-arachidonoylglycerol.

Structure[edit | edit source]

The CB1 receptor is a member of the rhodopsin-like G protein-coupled receptor family and is one of the most widely expressed GPCRs in the brain. It is composed of 472 amino acids and has a molecular weight of approximately 53 kDa.

Function[edit | edit source]

CB1 receptors play a role in the regulation of neurotransmission, appetite, pain, mood, and memory. They are also involved in mediating the psychoactive effects of cannabis. Activation of CB1 receptors inhibits the release of certain neurotransmitters, modulates postsynaptic neuron excitability, reduces neuronal firing, and decreases neurotransmitter release. In addition, CB1 receptors are involved in the alleviation of nausea and vomiting, and can reduce seizures and reduce anxiety.

Clinical significance[edit | edit source]

CB1 receptors are a target for the treatment of various disorders including obesity, neuropathic pain, spasticity, anxiety, and epilepsy. Drugs that selectively target CB1 receptors and modulate their activity are currently in development and have potential for the treatment of these and other disorders.