Abstract
Small molecule N/OFQ receptor antagonists were designed and synthesized to further investigate the therapeutic potential of N/OFQ receptor modulators. The resulting octahydrobenzimidazol-2-ones 14 and 23 show excellent antagonistic activity towards both N/OFQ and mu receptors with high affinity to the human N/OFQ receptor.
MeSH terms
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / pharmacology*
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Drug Design*
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Humans
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Narcotic Antagonists*
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Nociceptin Receptor
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Piperidines / chemical synthesis*
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Piperidines / pharmacology*
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Protein Binding
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Receptors, Opioid
Substances
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Benzimidazoles
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J 113397
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Narcotic Antagonists
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Piperidines
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Receptors, Opioid
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Nociceptin Receptor
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OPRL1 protein, human