Abstract
A pair of diastereomeric peptidomimetics based upon opioid receptor-binding pharmacophore models derived for a series of opioid tetrapeptides was synthesized. Both analogues display high opioid receptor affinity, moderate selectivity for the mu opioid receptor, and are potent, full agonists.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Drug Design
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Kinetics
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Opioid Peptides / chemical synthesis*
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Opioid Peptides / metabolism
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Opioid Peptides / pharmacology*
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Protein Conformation
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Receptors, Opioid, delta / agonists*
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Receptors, Opioid, delta / metabolism
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Receptors, Opioid, mu / agonists*
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Receptors, Opioid, mu / metabolism
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Opioid Peptides
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Receptors, Opioid, delta
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Receptors, Opioid, mu