Abstract
κ-Opioid receptor agonists with high selectivity over the μ-opioid receptor and peripheral selectivity are attractive targets in the development of drugs for pain. We have previously attempted to create novel analgesics with peripheral selective κ-opioid receptor agonist on the basis of TRK-820. In this study, we elucidated the biological properties of 17-hydroxy-cyclopropylmethyl and 10α-hydroxy derivatives. These compounds were found to have better κ-opioid receptor selectivity and peripheral selectivity than TRK-820.
Keywords:
TRK-820; analgesic; κ-opioid receptor; μ-opioid receptor.
MeSH terms
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Acetic Acid
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Analgesics / chemical synthesis
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Analgesics / chemistry
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Analgesics / pharmacology*
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Animals
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Dose-Response Relationship, Drug
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Drug Discovery*
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Male
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Mice
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Mice, Inbred ICR
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Models, Molecular
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Molecular Conformation
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Morphinans / chemical synthesis
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Morphinans / chemistry
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Morphinans / pharmacology*
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Pain / chemically induced
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Pain / drug therapy*
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Receptors, Opioid, kappa / agonists*
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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
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Morphinans
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Receptors, Opioid, kappa
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Spiro Compounds
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TRK 820
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Acetic Acid