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Titolo:
Pindolol antagonises G-protein activation at both pre- and postsynaptic serotonin 5-HT1A receptors: a [S-35]GTP gamma S autoradiography study
Autore:
Newman-Tancredi, A; Chaput, C; Touzard, M; Millan, MJ;
Indirizzi:
Inst Rech Servier, Dept Psychopharmacol, F-78290 Paris, France Inst Rech Servier Paris France F-78290 opharmacol, F-78290 Paris, France
Titolo Testata:
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
fascicolo: 4, volume: 363, anno: 2001,
pagine: 391 - 398
SICI:
0028-1298(200104)363:4<391:PAGAAB>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
IN-VIVO MICRODIALYSIS; DORSAL RAPHE NUCLEUS; FREELY-MOVING RATS; GAMMA-S-BINDING; FRONTAL-CORTEX; PHARMACOLOGICAL CHARACTERIZATION; ANTIDEPRESSANT ACTIVITY; REUPTAKE INHIBITOR; NEURONAL-ACTIVITY; MAJOR DEPRESSION;
Keywords:
[S-35]GTP gamma S; autoradiography; 5-HT1A receptors; G-protein; pindolol; depression; SSRI;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
67
Recensione:
Indirizzi per estratti:
Indirizzo: Millan, MJ Inst Rech Servier, Dept Psychopharmacol, 125 Chemin Ronde, F-78290 Paris, France Inst Rech Servier 125 Chemin Ronde Paris France F-78290 France
Citazione:
A. Newman-Tancredi et al., "Pindolol antagonises G-protein activation at both pre- and postsynaptic serotonin 5-HT1A receptors: a [S-35]GTP gamma S autoradiography study", N-S ARCH PH, 363(4), 2001, pp. 391-398

Abstract

The arylalkylamine, pindolol, may potentiate the clinical actions of antidepressant agents. Although it is thought to act via blockade of 5-HT1A autoreceptors, its efficacy at these sites remains controversial. Herein, we evaluated the actions of pindolol at 5-HT1A autoreceptors and specific populations of postsynaptic 5-HT1A receptors employing [S-35]GTP gammaS autoradiography, a measure of receptor-mediated G-protein activation. Both 8-OH-DPAT(1 muM) and 5-HT (10 muM) elicited a pronounced increase in [S-35]GTP gammaS binding in the dorsal raphe nucleus, which contains serotonergic cell bodies bearing 5-HT1A autoreceptors. Pindolol abolished their actions. In thedentate gyrus, lateral septum and entorhinal cortex, structures enriched in postsynaptic 5-HT1A receptors, 8-OH-DPAT (1 muM) and 5-HT (10 muM) also elicited a marked increase in [S-35]GTP gammaS binding which was likewise blocked by pindolol. The antagonism of 5-HT-induced [S-35]GTP gammaS labelling in the dentate gyrus was shown to be concentration-dependent, yielding a pIC(50) Of 5.82. Pindolol did not, itself, affect [S-35]GTP gammaS binding in any brain region examined. In conclusion, these data suggest that, as characterised by [S-35]GTP gammaS autoradiography, and compared with 5-HT and8-OH-DPAT, pindolol possesses low efficacy at both pre- and postsynaptic 5-HT1A receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/09/20 alle ore 07:55:36