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Titolo:
Analysis of [H-3] bremazocine binding in single and combinatorial opioid receptor knockout mice
Autore:
Simonin, F; Slowe, S; Becker, JAJ; Matthes, HWD; Filliol, D; Chluba, J; Kitchen, I; Kieffer, BL;
Indirizzi:
Univ Strasbourg 1, ESBS, CNRS, UPR 9050, F-67400 Strasbourg, France Univ Strasbourg 1 Strasbourg France F-67400 , F-67400 Strasbourg, France Univ Surrey, Sch Biol Sci, Pharmacol Res Grp, Guildford GU2 5XH, Surrey, England Univ Surrey Guildford Surrey England GU2 5XH ord GU2 5XH, Surrey, England Fac Pharm, CNRS, UMR 7514, F-67400 Illkirch, France Fac Pharm Illkirch France F-67400 RS, UMR 7514, F-67400 Illkirch, France
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2-3, volume: 414, anno: 2001,
pagine: 189 - 195
SICI:
0014-2999(20010302)414:2-3<189:AO[BBI>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; OPIATE BINDING; RAT-BRAIN; INDUCED ANALGESIA; MOUSE-BRAIN; SUBTYPES; SITES; PEPTIDES; KAPPA-1; DRUGS;
Keywords:
bremazocine; kappa(2)-opioid receptor; opioid-receptor knock-out mouse; opioid pharmacology;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Simonin, F Univ Strasbourg 1, ESBS, CNRS, UPR 9050, F-67400 Strasbourg, France Univ Strasbourg 1 Strasbourg France F-67400 trasbourg, France
Citazione:
F. Simonin et al., "Analysis of [H-3] bremazocine binding in single and combinatorial opioid receptor knockout mice", EUR J PHARM, 414(2-3), 2001, pp. 189-195

Abstract

Despite ample pharmacological evidence for the existence of multiple mu-. delta- and kappa -opioid receptor subtypes. only three genes encoding mu-(MOR), delta-(DOR) and kappa-(KOR) opioid receptor have been cloned. The KOR gene encodes kappa (1)-sites. which specifically bind arylacetamide compounds, and the possible existence of kappa -opioid receptor subtypes derived from another kappa -opioid-receptor gene, yet to be characterized, remains avery contentious issue. kappa (2)-Opioid receptors are described as binding sites typically labelled by the non-selective benzomorphan ligand [H-3]bremazocine in the presence of mu-, delta- and kappa (1)-opioid receptor blocking ligands. To investigate the genetic origin of kappa (2)-opioid receptors, we have carried out homogenate binding experiments with [H-3]bremazocine in brains of single MOR-, DOR-, KOR- and double MOR/DOR-deficient mice. Scatchard analysis showed that 68 +/- 12% of the binding sites arise from the MOR gene, 27 +/- 1% from the DOR gene and 14.5 +/- 0.2% from the KOR gene, indicating that the three known genes account for total [H-3]bremazocine binding. Experiments in the presence of mu-. delta- and kappa (1)-opioid receptor suppressor ligands further showed that non-kappa (1)-opioid receptorlabelling can be accounted for by binding to both the mu- and delta -opioid receptors. Finally, [H-3]bremazocine binding experiments performed on brain membranes from the triple MOR/DOR/KOR-deficient mice revealed a completeabsence of binding sites, confirming definitively that no additional gent:is required to explain the total population of [H-3]bremazocine binding sites. Altogether the data show that the putative kappa (2)-opioid receptors are in fact a mixed population of KOR, DOR and predominantly MOR gene products. (C) 2001 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 01:42:26