Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy

…, Z Wu, DA Henze, K Della Penna, R Desai…

文献索引：Trotter, B. Wesley; Nanda, Kausik K.; Burgey, Christopher S.; Potteiger, Craig M.; Deng, James Z.; Green, Ahren I.; Hartnett, John C.; Kett, Nathan R.; Wu, Zhicai; Henze, Darrell A.; Penna, Kimberly Della; Desai, Reshma; Leitl, Michael D.; Lemaire, Wei; White, Rebecca B.; Yeh, Suzie; Urban, Mark O.; Kane, Stefanie A.; Hartman, George D.; Bilodeau, Mark T. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2354 - 2358

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被引用次数: 28

摘要

A new series of imidazopyridine CB2 agonists is described. Structural optimization improved CB2/CB1 selectivity in this series and conferred physical properties that facilitated high in vivo exposure, both centrally and peripherally. Administration of a highly selective CB2 agonist in a rat model of analgesia was ineffective despite substantial CNS exposure, while administration of a moderately selective CB2/CB1 agonist exhibited significant analgesic ...