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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Trotter BW,Nanda KK,Burgey CS,Potteiger CM,Deng JZ,Green AI,Hartnett JC,Kett NR,Wu Z,Henze DA,Della Penna K,Desai R,Leitl MD,Lemaire W,White RB,Yeh S,Urban MO,Kane SA,Hartman GD,Bilodeau MTdoi
10.1016/j.bmcl.2011.02.082subject
Has Abstractpub_date
2011-04-15 00:00:00pages
2354-8issue
8eissn
0960-894Xissn
1464-3405pii
S0960-894X(11)00266-6journal_volume
21pub_type
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