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AM-630

AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB<sub>2</sub>, with a K<sub>i</sub> of 32.1&nbsp;nM at CB<sub>2</sub> and 165x selectivity over CB<sub>1</sub>, at which it acted as a weak partial agonist. It is used in the study of CB<sub>2</sub> mediated responses and has been used to investigate the possible role of CB<sub>2</sub> receptors in the brain. AM-630 is significant as one of the first indole derived cannabinoid ligands substituted on the 6-position of the indole ring, a position that has subsequently been found to be important in determining affinity and efficacy at both the CB<sub>1</sub> and CB<sub>2</sub> receptors, and has led to the development of many related derivatives.

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