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2007
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Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
Poitout, L., Brault, V., Sackur, C., Bernetiere, S., Camara, J., Plas, P., Roubert, P.
Journal
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Bioorg Med Chem Lett
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Species
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Analytes Measured
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cAMP
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Matrix Tested
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Cell lysates
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Abstract
A novel series of benzimidazoles was identified and optimized, leading to the discovery of potent and selective antagonists of the human melanocortin-4 receptor. In addition, compound 5i was shown to cross the blood-brain barrier after intravenous dosing in rats.
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