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

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 Lett

authors

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 MT

doi

10.1016/j.bmcl.2011.02.082

subject

Has Abstract

pub_date

2011-04-15 00:00:00

pages

2354-8

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00266-6

journal_volume

21

pub_type

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