Abstract
Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1.
MeSH terms
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Animals
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Behavior, Animal / drug effects
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Feeding Behavior / drug effects
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Conformation
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Pyridines / chemical synthesis*
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Pyridines / chemistry*
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Rats
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Rats, Sprague-Dawley
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Receptor, Cannabinoid, CB1 / agonists*
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Structure-Activity Relationship
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Temperature
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Toluene / chemistry
Substances
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Pyridines
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Receptor, Cannabinoid, CB1
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Toluene