Abstract
Several novel racemic aminotetralin derivatives have been prepared using a stereoselective aziridine ring opening reactions and were evaluated for their micro-opioid receptor binding affinity. Selectivity index towards other opioid receptors and antinociceptive activity in mice have been evaluated for the most potent derivatives.
MeSH terms
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Analgesics, Opioid / chemical synthesis*
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Analgesics, Opioid / pharmacology*
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Animals
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Indicators and Reagents
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Mice
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Pain Measurement / drug effects
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Receptors, Opioid, delta / drug effects
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Receptors, Opioid, delta / metabolism
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Receptors, Opioid, kappa / drug effects
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Receptors, Opioid, kappa / metabolism
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Receptors, Opioid, mu / drug effects*
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Stereoisomerism
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Structure-Activity Relationship
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Tetrahydronaphthalenes / chemical synthesis*
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Tetrahydronaphthalenes / pharmacology*
Substances
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Analgesics, Opioid
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Indicators and Reagents
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Receptors, Opioid, delta
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
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Tetrahydronaphthalenes