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Bioorg Med Chem Lett. 2012 Apr 1;22(7):2604-8. doi: 10.1016/j.bmcl.2012.01.121. Epub 2012 Feb 4.

Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB₂ receptor agonists for pain management.

Author information

1
Neurological Diseases Research, Global Pharmaceutical R&D, Abbott, 100 Abbott Park Road, Abbott Park, IL 60064, USA. derek.nelson@abbott.com

Abstract

SAR studies on a series of thiophene amide derivatives provided CB(2) receptor agonists. The activity of the compounds was characterized by radioligand binding determination, multiple functional assays, ADME, and pharmacokinetic studies. A representative compound with selectivity for CB(2) over CB(1) effectively produced analgesia in behavioral models of neuropathic, inflammatory, and postsurgical pain. Control experiments using a CB(2) antagonist demonstrated the efficacy in the pain models resulted from CB(2) agonism.

PMID:
22370265
DOI:
10.1016/j.bmcl.2012.01.121
[Indexed for MEDLINE]

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