The design of delta-selective opioid receptor antagonists.
Naltrexone-derived antagonists which are highly selective for delta opioid receptors have been designed using the message-address concept. The prototypical member of this series, naltrindole 1, possesses very high affinity and selectivity for delta receptors, and a closely related benzofuran analogue, NTB 2, is a selective delta 2 antagonist. The fact that 7-benzylidenenaltrexone (BNTX) was found to be a delta 1 antagonist suggests that the conformation of the putative delta address component (phenyl group) of BNTX plays a role in modulating delta subtype selectivity.
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis 55455.
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Portoghese
D000595:Amino Acid Sequence; D000818:Animals; D015195:Drug Design; D006801:Humans; D008968:Molecular Conformation; D008969:Molecular Sequence Data; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000737:chemistry / Q000494:pharmacology; D017465:Receptors, Opioid, delta / Q000037:antagonists & inhibitors* / Q000737:chemistry
D009292:Narcotic Antagonists; D017465:Receptors, Opioid, delta; D009271:Naltrexone; C055382:naltrindole