Abstract
Small peptidic kappa agonists were covalently linked to the reactive lysine of the CovX antibody to create compounds having potent activity at the kappa receptor with greatly extended half-life when compared to the parent peptide as exemplified by compound 20.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Analgesics / chemical synthesis*
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Analgesics / pharmacology
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Animals
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Antibodies / chemistry
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Arrestins / metabolism
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Azetidines / chemistry
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Cell Line, Tumor
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Drug Delivery Systems
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Half-Life
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Humans
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Immunoconjugates / chemistry*
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Immunoconjugates / pharmacology
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Ligands
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Opioid Peptides / chemical synthesis*
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Opioid Peptides / pharmacology
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Protein Transport / drug effects
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Rats
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Receptors, Opioid, kappa / agonists*
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Receptors, Opioid, kappa / metabolism
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Small Molecule Libraries / chemical synthesis*
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Small Molecule Libraries / pharmacology
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Structure-Activity Relationship
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beta-Arrestins
Substances
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2-azetidinone
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Analgesics
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Antibodies
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Arrestins
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Azetidines
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Immunoconjugates
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Ligands
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Opioid Peptides
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Receptors, Opioid, kappa
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Small Molecule Libraries
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beta-Arrestins