Abstract
By focusing on 4,5-epoxymorphinan, a traditional opioid skeleton but a new structure in the opioid kappa-agonist research field, and by rationally applying the 'message-address concept' and 'accessory site hypothesis,' we discovered a new chemical class opioid kappa-agonist, TRK-820 (1). Its development as an antipruritus is now in the final stage. Here, the full scope of its design, synthesis, and structure-activity relationship are described.
MeSH terms
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Analgesics, Opioid / chemical synthesis
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Analgesics, Opioid / chemistry
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Drug Design*
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Molecular Structure
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Morphinans / chemical synthesis
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Morphinans / chemistry
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Morphinans / pharmacology
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Receptors, Opioid, kappa / agonists*
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Receptors, Opioid, kappa / antagonists & inhibitors
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Receptors, Opioid, kappa / metabolism
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Spiro Compounds / chemical synthesis
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Spiro Compounds / chemistry
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Spiro Compounds / pharmacology
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Structure-Activity Relationship
Substances
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Analgesics, Opioid
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Morphinans
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Receptors, Opioid, kappa
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Spiro Compounds
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TRK 820