Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists
DOI: 10.1016/0165-6147(89)90267-8
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摘要: Abstract Metabolically stable receptor antagonists that are subtype selective indispensable pharmacological tools. In this article , Philip Portoghese describes the bivalent ligand approach to drug design which has resulted in development of several highly non-peptide opioid antagonists, such as κ-selective norbinaltorphimine and δ-selective naltrindole. Models used resemble Schwyzer's message-address concept originally described recognition elements peptide hormones; their success augurs well for possibility altering antagonist selectivity a predictable fashion by simulating portion address component with rigid moiety .
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