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Titolo:
DIFFERENTIAL-EFFECTS OF SYSTEMICALLY ADMINISTERED NOR-BINALTORPHIMINE(NOR-BNI) ON KAPPA-OPIOID AGONISTS IN THE MOUSE WRITHING ASSAY
Autore:
BROADBEAR JH; NEGUS SS; BUTELMAN ER; DECOSTA BR; WOODS JH;
Indirizzi:
UNIV MICHIGAN,DEPT PHARMACOL ANN ARBOR MI 48109 UNIV MICHIGAN,DEPT PSYCHOL ANN ARBOR MI 48109 NIDDK BETHESDA MD 20892
Titolo Testata:
Psychopharmacology
fascicolo: 3, volume: 115, anno: 1994,
pagine: 311 - 319
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; BETA-FUNALTREXAMINE; RECEPTOR SUBTYPES; OPIATE RECEPTORS; DELTA-RECEPTOR; BINDING-SITES; MORPHINE-LIKE; RAT-BRAIN; ANTAGONIST; ANTINOCICEPTION;
Keywords:
NOR-BINALTORPHIMINE; CI-977; U69,593; U50,488; BREMAZOCINE; ETHYLKETOCYCLAZOCINE; MR2034; MORPHINE; BW-373U86; BETA-FUNALTREXAMINE; KAPPA ANTAGONISTS; ACETIC ACID-INDUCED WRITHING; MICE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
49
Recensione:
Indirizzi per estratti:
Citazione:
J.H. Broadbear et al., "DIFFERENTIAL-EFFECTS OF SYSTEMICALLY ADMINISTERED NOR-BINALTORPHIMINE(NOR-BNI) ON KAPPA-OPIOID AGONISTS IN THE MOUSE WRITHING ASSAY", Psychopharmacology, 115(3), 1994, pp. 311-319

Abstract

The opioid antagonist effects of systemically administered nor-binaltorphimine (nor-BNI) were evaluated against the kappa agonists CI-977, U69,593, U50,488, ethylketocyclazocine (EKC), Mr2034 and bremazocine, the mu agonist morphine and the alkaloid delta agonist BW-373U86 in the acetic acid-induced writhing assay in mice. All eight agonists completely and dose-dependently inhibited writhing. Antagonism of CI-977 was apparent 1 h after administration of 32 mg/kg nor-BNI, peaking after4 h and was maintained for at least 4 weeks; no antagonist effects ofnor-BNI were apparent after 8 weeks. Nor-BNI (32 mg/kg) caused littleor no antagonism of morphine or BW-373U86 at 1 h and none at 24 h after nor-BNI administration. Subsequently, dose-effect curves for CI-977, U50,488, U69,593, EKC, Mr2034 and bremazocine were determined 24 h after pretreatment with 3.2, 10 and 32 mg/kg nor-BNI. Pretreatment with3.2 mg/kg nor-BNI produced significant antagonism of all six kappa agonists, suggesting that their antinociceptive effects were mediated atleast in part by nor-BNI-sensitive kappa receptors. At higher doses, nor-BNI dose-dependently shifted the agonist dose-effect curves of CI-977, U50,488, U69,593 and bremazocine, but not those of EKC and Mr2034, suggesting that the latter compounds may be producing effects via nor-BNI-insensitive receptors. Mu receptor involvement was demonstrated following a 24 h pretreatment with 32 mg/kg beta-FNA in combination with nor-BNI, which significantly increased the degree of antagonism of Mr2034 and EKC from that seen with nor-BNI alone. Hence, SC administered nor-BNI selectively antagonized agonist activity mediated through kappa-opioid receptors without differentiating between kappa subtypes. Nor-BNI also enabled the mu agonist activity of proposed kappa agonists to be measured.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 22:31:59