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GW842166 is a small molecule drug developed as a potent and selective agonist of the cannabinoid CB2 receptor, with a novel pyrimidine-based chemical structure. It exhibits strong analgesic, anti-inflammatory, and anti-hyperalgesic effects in animal models but lacks cannabis-like behavioral effects due to its extremely low affinity for the CB1 receptor. The compound was primarily investigated for the treatment of inflammatory pain and osteoarthritis by GlaxoSmithKline (now GSK). Clinical trials included studies in dental pain, musculoskeletal pain, osteoarthritis (including knee osteoarthritis), inflammation, and tobacco use disorder/smoking cessation. However, clinical efficacy was not demonstrated in acute dental pain settings compared to ibuprofen. Development has been discontinued for all indications[1][3][4][5][6].
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