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Titolo:
ELECTROPHYSIOLOGICAL AND NEUROCHEMICAL EVIDENCE THAT PINDOLOL HAS AGONIST PROPERTIES AT THE 5-HT1A AUTORECEPTOR IN-VIVO
Autore:
CLIFFORD EM; GARTSIDE SE; UMBERS V; COWEN PJ; HAJOS M; SHARP T;
Indirizzi:
UNIV OXFORD,RADCLIFFE INFIRM,DEPT CLIN PHARMACOL,WOODSTOCK RD OXFORD OX2 6HE ENGLAND UNIV OXFORD,RADCLIFFE INFIRM,DEPT CLIN PHARMACOL OXFORD OX2 6HE ENGLAND WARNEFORD HOSP,DEPT PSYCHIAT,PSYCHOPHARMACOL RES UNIT OXFORD OX3 7JX ENGLAND
Titolo Testata:
British Journal of Pharmacology
fascicolo: 1, volume: 124, anno: 1998,
pagine: 206 - 212
SICI:
0007-1188(1998)124:1<206:EANETP>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-ADRENOCEPTOR ANTAGONISTS; BINDING-SITES; RAT-BRAIN; 5-HYDROXYTRYPTAMINE RELEASE; ANTICONFLICT ACTIVITY; ANTIDEPRESSANT DRUGS; RECEPTOR ACTIVATION; ADENYLATE-CYCLASE; MAJOR DEPRESSION; BODY-TEMPERATURE;
Keywords:
PINDOLOL; 5-HT1A RECEPTOR; ANTIDEPRESSANTS; DRN; MICRODIALYSIS; ELECTROPHYSIOLOGY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
E.M. Clifford et al., "ELECTROPHYSIOLOGICAL AND NEUROCHEMICAL EVIDENCE THAT PINDOLOL HAS AGONIST PROPERTIES AT THE 5-HT1A AUTORECEPTOR IN-VIVO", British Journal of Pharmacology, 124(1), 1998, pp. 206-212

Abstract

1 It has been hypothesized that 5-HT1A autoreceptor antagonists may enhance the therapeutic efficacy of SSRIs and other antidepressants. Although early clinical trials with the beta-adrenoceptor/5-HT1 ligand, pindolol, were promising, the results of recent more extensive trials have been contradictory. Here we investigated the actions of pindolol at the 5-HT1A autoreceptor by measuring its effect on 5-HT neuronal activity and release in the anaesthetized rat. 2 Pindolol inhibited the electrical activity of 5-HT neurones in the dorsal raphe nucleus (DRN). This effect was observed in the majority of neurones tested (10/16),was dose-related (0.2-1.0 mg kg(-1), i.v.), and was reversed by the 5-HT1A receptor antagonist, WAY 100635 (0.1 mg kg(-1), i.v.), in 6/7 cases tested. 3 Pindolol also inhibited 5-HT neuronal activity when applied microiontophoretically into the DRN in 9/10 neurones tested. This effect of pindolol was current-dependent and blocked by co-applicationof WAY 100635 (3/3 neurones tested). 4 In microdialysis experiments, pindolol caused a dose-related (0.8 and 4 mg kg(-1), i.v.) fall in 5-HT levels in dialysates from the frontal cortex (under conditions wherethe perfusion medium contained 1 mu M citalopram). In rats pretreatedwith WAY 100635 (0.1 mg kg(-1), i.v.), pindolol (4 mg kg(-1), i.v.) did not decrease, but rather increased 5-HT levels. 5 We conclude that,under the experimental conditions used in this study, pindolol displays agonist effects at the 5-HT1A autoreceptor. These data are relevantto previous and ongoing clinical trials of pindolol in depression which are based on the rationale that the drug is an effective 5-HT1A autoreceptor antagonist.

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Documento generato il 05/07/20 alle ore 21:24:36