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AM630 (6-Iodopravadoline) is a potent and selective small molecule ligand that acts primarily as an inverse agonist and competitive antagonist at the cannabinoid receptor CB2, with high selectivity over the CB1 receptor. It exhibits a Ki of approximately 31–32 nM for CB2 and is about 165 times more selective for CB2 than for CB1, where it acts as a weak partial agonist. AM630 has been widely used in research to study the physiological roles of cannabinoid receptors—especially CB2—in various systems including pain modulation, inflammation, and neurobiology. It also displays activity at TRPA1 channels in sensory neurons. The compound was one of the first indole-derived cannabinoid ligands substituted at the 6-position of the indole ring—a modification important for affinity and efficacy at both major cannabinoid receptors[1][3][4][7].
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