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Titolo:
AUTORADIOGRAPHY OF SEROTONIN 5-HT1A RECEPTOR-ACTIVATED G-PROTEINS IN GUINEA-PIG BRAIN SECTIONS BY AGONIST-STIMULATED [S-35] GTP-GAMMA-S BINDING
Autore:
DUPUIS DS; PALMIER C; COLPAERT FC; PAUWELS PJ;
Indirizzi:
CTR RECH PIERRE FABRE,DEPT CELLULAR & MOL BIOL,17 AVE JEAN MOULIN F-81106 CASTRES FRANCE CTR RECH PIERRE FABRE,DEPT CELLULAR & MOL BIOL F-81106 CASTRES FRANCE
Titolo Testata:
Journal of neurochemistry
fascicolo: 3, volume: 70, anno: 1998,
pagine: 1258 - 1268
SICI:
0022-3042(1998)70:3<1258:AOS5RG>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
ADENYLATE-CYCLASE ACTIVITY; RAT HIPPOCAMPAL MEMBRANES; GAMMA-S BINDING; PHARMACOLOGICAL CHARACTERIZATION; SELECTIVE RADIOLIGAND; MEDIATED INHIBITION; INVITRO BINDING; SITES; SUBTYPES; CELLS;
Keywords:
SEROTONIN 5-HT1A RECEPTOR; G PROTEIN ACTIVATION; [S-35] GTP-GAMMA-S BINDING AND AUTORADIOGRAPHY; 5-HT1 LIGANDS; GUINEA PIG BRAIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
48
Recensione:
Indirizzi per estratti:
Citazione:
D.S. Dupuis et al., "AUTORADIOGRAPHY OF SEROTONIN 5-HT1A RECEPTOR-ACTIVATED G-PROTEINS IN GUINEA-PIG BRAIN SECTIONS BY AGONIST-STIMULATED [S-35] GTP-GAMMA-S BINDING", Journal of neurochemistry, 70(3), 1998, pp. 1258-1268

Abstract

G protein activation mediated by serotonin 5-HT1A and 5-HT1B/D receptors in guinea pig brain was investigated by using quantitative autoradiography of agonist-stimulated [S-35]GTP gamma S binding to brain sections, [S-35]GTP gamma S binding was stimulated by the mixed 5-HT1A/5-HT1B/D agonist L694247 in brain structures enriched in 5-HT1A binding sites, i.e., hippocampus (+140 +/- 14%), dorsal raphe (+70 +/- 8%), lateral septum (+52 +/- 12%), cingulate (+36 +/- 8%), and entorhinal cortex (+34 +/- 5%), L694247 caused little or no stimulation of [S-35] GTPgamma S binding in brain regions with high densities of 5-HT1B/D binding sites (e.g., substantia nigra, striatum, central gray, and dorsal subiculum). The [S-35]GTP gamma S binding response was antagonized by WAY100635 (10 mu M) and methiothepin (10 mu M). In contrast, the 5-HT1B inverse agonist SB224289 (10 mu M) did not affect the L694247-mediated [S-35]GTP gamma S binding response, and the mixed 5-HT1B/D antagonist GR127935 (10 mu M) yielded a partial blockade. The distribution pattern of the [S-35]GTP gamma S binding response and the antagonist profile suggest the L694247-mediated response in guinea pig brain to be mediated by 5-HT1A receptors. In addition to L694247, 8-hydroxy-2-(di-n-propylamino) tetralin, and flesinoxan also stimulated [S-35]GTP gamma S binding; their maximal responses varied between 46 and 52% compared with L694247, irrespective of the brain structure being considered. Sumatriptan, rizatriptan, and zolmitriptan (10 mu M) stimulated [S-35]GTP gamma S binding in the hippocampus by 20-50%, Naratriptan, CP122638,and dihydroergotamine stimulated [S-35]GTP gamma S binding to a similar level as L694247 in hippocampus, lateral septum, and dorsal raphe. It appears that under the present experimental conditions, G protein activation through 5-HT1A but not 5-HT1B/D receptors can be measured inguinea pig brain sections.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 10:31:32