A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.
Olmsted
S L
SL
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis 55455.
Takemori
A E
AE
Portoghese
P S
PS
D000818:Animals; D006168:Guinea Pigs; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D009019:Morphinans / Q000494:pharmacology*; D009271:Naltrexone / Q000031:analogs & derivatives*; D009292:Narcotic Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D017465:Receptors, Opioid, delta / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017473:Receptors, Opioid, kappa / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D007211:Indoles; D009019:Morphinans; D009292:Narcotic Antagonists; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D009271:Naltrexone; C055382:naltrindole