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Titolo:
EFFECTS OF THE ALKYLATING AGENT EEDQ ON REGULATORY G-PROTEINS AND RECOVERY OF AGONIST AND ANTAGONIST ALPHA(2)-ADRENOCEPTOR BINDING-SITES INRAT-BRAIN
Autore:
RIBAS C; MIRALLES A; ESCRIBA PV; GARCIASEVILLA JA;
Indirizzi:
UNIV ILLES BALEARS,DEPT BIOL,CSIC,INST NEUROBIOL RAMON & CAJAL,LAB NEUROPHARMACOL E-07071 PALMA DE MALLORCA BALEARS SPAIN UNIV ILLES BALEARS,DEPT BIOL,CSIC,INST NEUROBIOL RAMON & CAJAL,LAB NEUROPHARMACOL,ASSOCIATE UNIT E-07071 PALMA DE MALLORCA BALEARS SPAIN
Titolo Testata:
European journal of pharmacology
fascicolo: 1, volume: 351, anno: 1998,
pagine: 145 - 154
SICI:
0014-2999(1998)351:1<145:EOTAAE>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
ADRENERGIC-RECEPTOR SUBTYPES; LONG-TERM TREATMENT; ADENYLATE-CYCLASE; H-3 RX821002; ALPHA-2-ADRENERGIC RECEPTORS; IRREVERSIBLE INACTIVATION; GUANINE-NUCLEOTIDE; IN-VIVO; TURNOVER; N-ETHOXYCARBONYL-2-ETHOXY-1,2-DIHYDROQUINOLINE;
Keywords:
ALPHA(2)-ADRENOCEPTOR TURNOVER; [H-3]UK 14304 (BROMOXIDINE); [H-3]RX 821002 (2-METHOXY IDAZOXAN); G PROTEIN; EEDQ (N-ETHOXYCARBONYL-2-ETHOXY-1,2-DIHYDROQUINOLINE);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
60
Recensione:
Indirizzi per estratti:
Citazione:
C. Ribas et al., "EFFECTS OF THE ALKYLATING AGENT EEDQ ON REGULATORY G-PROTEINS AND RECOVERY OF AGONIST AND ANTAGONIST ALPHA(2)-ADRENOCEPTOR BINDING-SITES INRAT-BRAIN", European journal of pharmacology, 351(1), 1998, pp. 145-154

Abstract

The aim of this study was to assess the effect of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)-induced alpha(2)-adrenoceptor inactivation on regulatory G proteins and the recovery of agonist and antagonist binding sites. EEDQ induced a rapid increase in the abundance ofrat brain cortical G alpha(i1/2) proteins (30% at 6 h) which reached a maximum at 4 days (45%) and which then slowly returned (7-30 days) to control values. EEDQ did not alter significantly the levels of G alpha(i3) and G alpha(o) proteins. By using the standard monoexponential model, the analysis of the recovery of alpha(2)-adrenoceptor density (6 h-30 days) with [H-3]UK 14304 (bromoxidine) and [H-3]RX 821002 (2-metoxy idazoxan) in the cerebral cortex did not reveal differences in receptor turnover parameters. However, the recovery of [H-3]UK 14304 binding fitted best to a new biphasic recovery model, suggesting the existence of two distinct phases of recovery of agonist sites (r(1) and r(2) = 15.7 and 7.4 fmol mg protein(-1) day(-1); k(1) and k(2) = 0.51 and 0.25 day(-1); (t(1/2))(1) and (t(1/2))(2) = 1.4 and 2.7 days). In contrast, the recovery of [H-3]RX 821002 antagonist sites did not fit tothe biphasic model (r = 8.1, k = 0.14, t(1/2) = 4.9). Because agonistbinding requires coupling to G proteins, the present results suggest that the rapid over-expression of G alpha(i1/2) proteins induced by EEDQ is related to the biphasic recovery of [H-3]UK 14304 binding. The possible implication of the faster recovery of alpha(2)-adrenoceptor function after EEDQ inactivation is discussed. (C) 1998 Elsevier ScienceB.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/11/20 alle ore 16:29:32