Identity of the putative delta1-opioid receptor as a delta-kappa heteromer in the mouse spinal cord.
In view of the co-localization of spinal delta- and kappa-opioid receptors, we have investigated the interaction of selective opioid receptor agonists and antagonists in the spinal cord of mice in order to determine if these receptors are organized as heteromers. The finding that norbinaltorphimine (kappa) antagonized [D-Pen(2,5)]enkephalin (delta(1)), but not deltorphin II (delta(2)), strongly suggests that the putative delta(1)-subtype is a delta-kappa heteromer. Studies with selective opioid receptor (ant)agonists support this conclusion.
Portoghese
Philip S
PS
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard Street, S.E., Minneapolis, MN 55455, USA. porto001@umn.edu
Lunzer
Mary M
MM
D000818:Animals; D001597:Benzylidene Compounds / Q000494:pharmacology; D004399:Dynorphins / Q000276:immunology; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / Q000494:pharmacology; D020881:Enkephalin, D-Penicillamine (2,5)- / Q000494:pharmacology; D007106:Immune Sera / Q000494:pharmacology; D051379:Mice; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology; D017465:Receptors, Opioid, delta / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D017473:Receptors, Opioid, kappa / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000037:antagonists & inhibitors; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000494:pharmacology; D013116:Spinal Cord / Q000187:drug effects / Q000378:metabolism*
D001597:Benzylidene Compounds; D007106:Immune Sera; D009842:Oligopeptides; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; C049352:phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide; C068868:naltrindole benzofuran; C060209:deltorphin II, Ala(2)-; C077358:7-benzylidenenaltrexone; C051844:norbinaltorphimine; D013004:Somatostatin; D009271:Naltrexone; D004399:Dynorphins; D020881:Enkephalin, D-Penicillamine (2,5)-