Cannabinoid receptors and other central neural targets

Cannabinoid receptors and other central neural targets refers to a heterogeneous group of molecular entities involved in the endocannabinoid system and related neuromodulatory pathways within the central nervous system (IUPHAR/BPS). The primary components are the G protein-coupled receptors Cannabinoid receptor 1 (CB1) and Cannabinoid receptor 2 (CB2), which are critical for maintaining physiological homeostasis (UniProt P21554, P34972). CB1 is predominantly expressed in the brain and modulates the release of neurotransmitters like GABA and glutamate, while CB2 is primarily associated with neuroimmune functions (PubMed: 21295074). The category also encompasses other targets such as the orphan receptor GPR55, transient receptor potential (TRP) channels like TRPV1, and metabolic enzymes like fatty acid amide hydrolase (FAAH) (StatPearls: NBK546642). Drugs interacting with these targets, including Delta-9-tetrahydrocannabinol (THC) and Cannabidiol (CBD), are utilized to treat chronic pain, spasticity in multiple sclerosis, and refractory epilepsy (FDA: Epidiolex Label). However, therapeutic application is often complicated by psychoactive side effects and complex regulatory roles across different brain regions (PubMed: 28861491).

Other names

Endocannabinoid system targetsCNS cannabinoid-related targetsCannabinoid-sensitive neural receptors

Agonism or antagonism of CB1 and CB2 receptors, modulation of non-canonical GPCRs (e.g., GPR55), activation or desensitization of ion channels (e.g., TRPV1), and inhibition of endocannabinoid degradation enzymes (e.g., FAAH).