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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.
Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively .
CB-25 is a partial agonist of the CB1 cannabinoid receptor. It has been shown to enhance Forskolin-induced cAMP formation specifically in cancer cells, while not affecting hCB1-CHO cells. This compound serves as a valuable tool for investigating the role of cannabinoid signaling pathways in cancer biology and related research applications.
O-1269 is a partial agonist of cannabinoid receptor 1 (CB1R), displaying a binding affinity characterized by a Ki value of 32 nM. This compound exhibits significant analgesic effects, making it a valuable tool for investigations into pain modulation and cannabinoid receptor signaling pathways. Its application in research may provide insights into therapeutic strategies targeting CB1R-related conditions.
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