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Bioorg Med Chem Lett. 2011 Apr 15;21(8):2354-8. doi: 10.1016/j.bmcl.2011.02.082. Epub 2011 Mar 1.

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

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Boston, MA, USA. bwesley_trotter@merck.com

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.

PMID:
21420860
DOI:
10.1016/j.bmcl.2011.02.082
[Indexed for MEDLINE]

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