Abstract
The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.
MeSH terms
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Benzimidazoles / chemical synthesis
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Benzimidazoles / chemistry*
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Binding, Competitive
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Cannabinoid Receptor Modulators / chemistry
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Cannabinoids / chemistry
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Chemistry, Pharmaceutical / methods
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Drug Design
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Humans
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Models, Chemical
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Receptor, Cannabinoid, CB1 / chemistry
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Receptor, Cannabinoid, CB2 / chemistry*
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Receptors, Cannabinoid / chemistry
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Structure-Activity Relationship
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Technology, Pharmaceutical / methods
Substances
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Benzimidazoles
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Cannabinoid Receptor Modulators
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Cannabinoids
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Receptor, Cannabinoid, CB1
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Receptor, Cannabinoid, CB2
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Receptors, Cannabinoid
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benzimidazole