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Titolo:
ACUTE AND CHRONIC EFFECTS OF RESERPINE ON BIOCHEMICAL AND FUNCTIONAL PARAMETERS OF CENTRAL AND PERIPHERAL ALPHA-2-ADRENOCEPTORS
Autore:
UGEDO L; GARRO MA; PINEDA J; GIRALT MT; MIRALLES A; OLMOS G; GARCIASEVILLA JA; MENARGUES A; OBACH R;
Indirizzi:
UNIV ILLES BALEARS,DEPT BIOL FONAMENTAL & CIENCIES SALUT,NEUROFARMACOL LAB,CRA VALLDEMOSSA KM 75 E-07071 PALMA DE MALLORCA SPAIN UNIV ILLES BALEARS,DEPT BIOL FONAMENTAL & CIENCIES SALUT,NEUROFARMACOL LAB,CRA VALLDEMOSSA KM 75 E-07071 PALMA DE MALLORCA SPAIN UNIV BASQUE COUNTRY,FAC MED,DEPT PHARMACOL LLEIDA SPAIN SA LASA LABS,RES DEPT S FELIU LLOBREGAT SPAIN
Titolo Testata:
European journal of pharmacology
fascicolo: 1-3, volume: 239, anno: 1993,
pagine: 149 - 157
SICI:
0014-2999(1993)239:1-3<149:AACEOR>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
PERFORMANCE LIQUID-CHROMATOGRAPHY; AMINO-ACID DECARBOXYLASE; RAT CEREBRAL-CORTEX; NERVOUS-SYSTEM; 3,4-DIHYDROXYPHENYLACETIC ACID; ALPHA-ADRENORECEPTORS; ANTIDEPRESSANT DRUGS; HOMOVANILLIC-ACID; MAJOR DEPRESSION; BINDING-SITES;
Keywords:
ALPHA-2-ADRENOCEPTORS; BRAIN (RAT); VAS DEFERENS (RAT); [H-3]UK-14304; [H-3]RX-821002; RESERPINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
L. Ugedo et al., "ACUTE AND CHRONIC EFFECTS OF RESERPINE ON BIOCHEMICAL AND FUNCTIONAL PARAMETERS OF CENTRAL AND PERIPHERAL ALPHA-2-ADRENOCEPTORS", European journal of pharmacology, 239(1-3), 1993, pp. 149-157

Abstract

The specific binding of the agonist, [H-3]UK 14304, and of the antagonist, [H-3]RX 821002, to rat brain membranes, as well as clonidine-induced mydriasis, clonidine-induced inhibition and idazoxan-induced stimulation of brain 3,4-dihydroxyphenylalanine (DOPA) synthesis, and clonidine and UK 14304-induced inhibition of twitch responses in the vas deferens were used to evaluate the affinity and sensitivity of central and peripheral alpha2-adrenoceptors after various treatments with reserpine. Treatment with reserpine (0.25 mg/kg s.c., every 48 h) for 4, 11 and 18 days induced consistent and significant increases in the affinity (K(D) values) of [H-3]UK 14304 for the cortical alpha2-adrenoceptor with no change in receptor density. Chronic treatment with reserpine also resulted in a greater affinity of (-)-adrenaline for the high-affinity state of the alpha2-adrenoceptor when the catecholamine competed with the binding of [H-3]RX 821002 to cortical membranes. In line with these radioligand binding data, various functional responses mediated by central and peripheral alpha2-adrenoceptors were found to be potentiated after repeated treatment with reserpine. Thus, the inhibitory alpha2-autoreceptor that modulates the synthesis of brain noradrenaline and the central postsynaptic inhibitory alpha2-adrenoceptor that induces mydriasis displayed greater responses in vivo after chronic treatment with reserpine. Short-term and chronic treatments with reserpine also increased the sensitivity of peripheral presynaptic alpha2-adrenoceptors in the vas deferens. The results indicated that chronic treatment with a low dose of reserpine. which results in prolonged noradrenaline depletion (greater than 85%), induces biochemical (increased affinity of agonists for the high-affinity state of the receptor) and invivo functional supersensitivity of pre- and postsynaptic alpha2-adrenoceptors in the rat brain.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 07:59:59