| Literature DB >> 21420860 |
B Wesley Trotter1, Kausik K Nanda, Christopher S Burgey, Craig M Potteiger, James Z Deng, Ahren I Green, John C Hartnett, Nathan R Kett, Zhicai Wu, Darrell A Henze, Kimberly Della Penna, Reshma Desai, Michael D Leitl, Wei Lemaire, Rebecca B White, Suzie Yeh, Mark O Urban, Stefanie A Kane, George D Hartman, Mark T Bilodeau.
Abstract
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 effects.Entities:
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Year: 2011 PMID： 21420860 DOI： 10.1016/j.bmcl.2011.02.082
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823