Abstract
Opioid compounds with mixed micro agonist/delta antagonist properties could be used as analgesics with low propensity to induce tolerance and dependence. Here we report the synthesis of a new designed multiple ligand deriving from the micro selective agonist endomorphin-2 and the delta selective antagonist pharmacophore Dmt-Tic. As predicted, the resulting bivalent ligand showed a micro agonist/delta antagonist profile deriving from the corresponding activities of each pharmacophore.
Publication types
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Research Support, N.I.H., Intramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Dipeptides / chemical synthesis*
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Dipeptides / chemistry
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Dipeptides / pharmacology*
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Drug Design
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Ligands
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Molecular Structure
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Receptors, Opioid, delta / antagonists & inhibitors*
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Receptors, Opioid, mu / agonists*
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis*
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Tetrahydroisoquinolines / chemistry
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Tetrahydroisoquinolines / pharmacology*
Substances
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2',6'-dimethyltyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
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Dipeptides
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Ligands
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Oligopeptides
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Receptors, Opioid, delta
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Receptors, Opioid, mu
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Tetrahydroisoquinolines
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endomorphin 2