Abstract
A structurally unique and new class of opioid receptor antagonists (OpRAs) that bear no structural resemblance with morphine or endogenous opioid peptides has been discovered. A series of carboxamido-biaryl ethers were identified as potent receptor antagonists against mu, kappa and delta opioid receptors. The structure-activity relationship indicated para-substituted aryloxyaryl primary carboxamide bearing an amine tether on the distal phenyl ring was optimal for potent in vitro functional antagonism against three opioid receptor subtypes.
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Drug Design
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Ethers / chemical synthesis*
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Ethers / pharmacology*
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Guanosine 5'-O-(3-Thiotriphosphate) / antagonists & inhibitors
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Humans
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Molecular Conformation
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Narcotic Antagonists*
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Receptors, Opioid, delta / antagonists & inhibitors
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Receptors, Opioid, kappa / antagonists & inhibitors
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Receptors, Opioid, mu / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Ethers
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Narcotic Antagonists
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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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Guanosine 5'-O-(3-Thiotriphosphate)