Characterization of kappa and delta opioid receptors in isolated organs by using type/subtype selective agonists and antagonists.
BACKGROUND
The kappa and delta opioid receptors were characterized in longitudinal muscle strip of guinea-pig ileum (GPI, mu, kappa), mouse (MVD, delta, mu, kappa) and rabbit (LVD, kappa) vas deferens and rabbit ear artery (ART, delta, kappa) with particular attention to the presence of receptor subtypes.


METHODS
For this purpose, type/subtype selective agonist and antagonist were used such as [D-Ala2, D-Leu5]-enkephalin (delta agonist) [D-Pen2,5]-enkephalin (delta 1 agonist), deltorphin II (delta 2 agonist) naltriben (NTB, delta 2 antagonist), BOC-YPGFLT(OtBu) (delta antagonist) on the one hand and ethylketocyclazocine (EKC, kappa/(agonist), PD-117 302 (kappa 1 agonist), [Met5]-enkephalin-Arg6, Phe7 (ME-RF, delta/kappa 2/(agonist) and its amide ME-RF-NH2, kappa 2/(agonist), naltrexone (NTX, mu > delta = kappa antagonist) and norbinaltorphimine (nBNI, kappa antagonist) on the other hand.


CONCLUSIONS
In MVD the Ke of NTB against different (agonists revealed no receptor type heterogeneity. In LVD the Ke of nBNI but not of NTX against EKC versus the ones against ME-RF and ME-RF-NH2 indicated inhomogenous (receptor population. The (receptor antagonist BOC-YPGFLT(OtBu) antagonized the action of ME-RF-NH2 in ART but not in MVD or LVD indicating a special receptor subtype in ART (kappa, possibly delta).
Makó
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Department of Pharmacology and Pharmacotherapy, Semmelweis University, H-1445, Budapest, P.O.B. 370, Hungary. ronand@pharma.sote.hu
Rónai
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D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D004423:Ear / Q000473:pathology; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / Q000494:pharmacology; D016308:Enkephalin, Leucine-2-Alanine / Q000494:pharmacology; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives* / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000378:metabolism; D008297:Male; D051379:Mice; D009132:Muscles / Q000378:metabolism; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology; D011817:Rabbits; D017465:Receptors, Opioid, delta / Q000819:agonists / Q000037:antagonists & inhibitors / Q000096:biosynthesis*; D017473:Receptors, Opioid, kappa / Q000819:agonists / Q000037:antagonists & inhibitors / Q000096:biosynthesis*; D013997:Time Factors; D014649:Vas Deferens / Q000378:metabolism
D000701:Analgesics, Opioid; D009292:Narcotic Antagonists; D010455:Peptides; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; C068868:naltrindole benzofuran; D004744:Enkephalin, Methionine; D009271:Naltrexone; D016308:Enkephalin, Leucine-2-Alanine; C027511:enkephalin-Met, Arg(6)-Phe(7)-