Abstract
The design, synthesis and pharmacological evaluation of a novel class of Dmt-Tic dipeptide analogues are described. These resulting analogues bearing different C-terminal functionalities were found to bind to the human delta receptor with high affinity. One specific class of dipeptides bearing urea/thiourea functionalities showed partial to full activation of the delta receptor. Several dipeptides also showed good binding affinities with full activation of the human kappa receptor, a novel property for those ligands.
MeSH terms
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Dipeptides / chemical synthesis*
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Dipeptides / chemistry
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Dipeptides / metabolism
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Humans
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Isoquinolines / chemistry*
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Receptors, Opioid, delta / agonists
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Receptors, Opioid, delta / metabolism*
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Receptors, Opioid, kappa / agonists
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Receptors, Opioid, kappa / metabolism*
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Receptors, Opioid, mu / agonists
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Receptors, Opioid, mu / metabolism*
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Tetrahydroisoquinolines*
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Tyrosine / analogs & derivatives
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Tyrosine / chemistry*
Substances
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Dipeptides
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Isoquinolines
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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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Tetrahydroisoquinolines
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2',6'-dimethyltyrosine
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1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
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Tyrosine