Cannabinoid receptors and Fatty acid amide hydrolase (FAAH) (CB receptors and FAAH)

The endocannabinoid system (ECS) is a complex cell-signaling network comprising cannabinoid receptors (primarily CB1 and CB2) and the enzymes responsible for the synthesis and degradation of endocannabinoids, such as Fatty Acid Amide Hydrolase (FAAH) [4, 13]. CB1 receptors are predominantly found in the central nervous system and regulate neurotransmitter release, while CB2 receptors are mainly expressed in immune cells and modulate inflammatory responses [9, 18]. FAAH is the primary enzyme responsible for the hydrolysis of anandamide (AEA), a key endocannabinoid [1, 14]. Pharmacological modulation of this system involves direct activation or blockade of receptors, or indirect enhancement of endocannabinoid tone by inhibiting FAAH [4, 17]. This system plays a critical role in pain perception, mood regulation, appetite, and neuroprotection, making it a significant target for treating chronic pain, neurodegenerative diseases, and metabolic disorders [3, 15]. However, therapeutic development has faced challenges, including psychiatric side effects from CB1 antagonism and safety concerns in clinical trials of certain FAAH inhibitors [5, 6].

Other names

Endocannabinoid systemECSCannabinoid receptor 1Cannabinoid receptor 2Fatty acid amide hydrolaseCB1CB2FAAH

Drugs targeting this system act through direct agonism or antagonism of the G protein-coupled cannabinoid receptors (CB1 and CB2) or through the inhibition of the enzyme Fatty Acid Amide Hydrolase (FAAH), which increases the levels of the endocannabinoid anandamide [1, 4, 9].