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Cannabinoid receptor agonists, antagonists and inverse agonists act on the CB1 and CB2 receptors. Cannabinoid receptor 1 (CB1) was cloned from rat brain in 1990 and shown to be a G protein-coupled receptor. Cannabinoid receptor 2 (CB2) followed in 1993 as a peripheral receptor found in immune cells and tissues such as spleen. CB1 is abundant in the central nervous system, so the two subtypes are studied in neuroscience and immunology. WIN 55,212-2 mesylate activates both receptors, while AM251 blocks CB1 and AM630 blocks CB2. PF-3845 inhibits fatty acid amide hydrolase (FAAH), the enzyme that breaks down fatty acid amide endocannabinoids.
BB-22 is a potent CB1 receptor ligand that acts as a dopamine activator. It exhibits a high affinity for CB1 receptors with a Ki value of 0.11 nM and demonstrates effective activation with an EC50 value of 2.9 nM. This compound may be valuable in studying the roles of endocannabinoid and dopaminergic systems in various neurological and psychiatric disorders.
AM841 is an electrophilic ligand that acts as a high-affinity activator of the CB1 cannabinoid receptor. By covalently binding to a cysteine residue in helix six, AM841 effectively reduces Forskolin-stimulated cAMP accumulation and has been shown to slow gastrointestinal motility. This compound is useful for research applications investigating cannabinoid receptor signaling and its physiological effects.
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