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Bioorg Med Chem Lett. 2011 Apr 15;21(8):2359-64. doi: 10.1016/j.bmcl.2011.02.078. Epub 2011 Feb 26.

Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point PA, United States. peter_manley@merck.com

Abstract

A novel series of decahydroquinoline CB2 agonists is described. Optimization of the amide substituent led to improvements in CB2/CB1 selectivity as well as physical properties. Two key compounds were examined in the rat CFA model of acute inflammatory pain. A moderately selective CB2 agonist was active in this model. A CB2 agonist lacking functional CB1 activity was inactive in this model despite high in vivo exposure both peripherally and centrally.

PMID:
21420857
DOI:
10.1016/j.bmcl.2011.02.078
[Indexed for MEDLINE]

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