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Titolo:
DIMERIZATION OF 8-OH-DPAT INCREASES ACTIVITY AT SEROTONIN 5-HT1A RECEPTORS
Autore:
PAUWELS PJ; DUPUIS DS; PEREZ M; HALAZY S;
Indirizzi:
CTR RECH PIERRE FABRE,DEPT BIOL CELLULAIRE & MOL,17 AVE JEAN MOULIN F-81106 CASTRES FRANCE CTR RECH PIERRE FABRE,DIV CHIM MED 4 F-81106 CASTRES FRANCE
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 4, volume: 358, anno: 1998,
pagine: 404 - 410
SICI:
0028-1298(1998)358:4<404:DO8IAA>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
GAMMA-S BINDING; PROTEIN ALPHA-SUBUNITS; C6-GLIAL CELL-LINES; BIVALENT LIGANDS; OPIOID RECEPTOR; HUMAN 5-HT1A-RECEPTORS; AGONIST EFFICACY; INVERSE AGONIST; ACTIVATION; EXPRESSION;
Keywords:
5-HT1A, 5-HT1B AND 5-HT1D RECEPTOR; 8-OH-DPAT DIMER; BIVALENT LIGAND; [S-35] GTP-GAMMA-S BINDING AND AUTORADIOGRAPHY; GUINEA-PIG BRAIN; RECOMBINANT CELL LINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
P.J. Pauwels et al., "DIMERIZATION OF 8-OH-DPAT INCREASES ACTIVITY AT SEROTONIN 5-HT1A RECEPTORS", Naunyn-Schmiedeberg's archives of pharmacology, 358(4), 1998, pp. 404-410

Abstract

[S-35]GTP gamma S binding responses can be used to measure differences between the intrinsic activity of ligands at human 5-hydroxytrypamine-(1A) (h 5-HT1A) receptors expressed in recombinant cell lines. The maximal [S-35]GTP gamma S binding response to 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) was lower than that to 5-HT in a recombinantC6-glial membrane preparation and dependent on the GDP concentration:it was attenuated by about 60% vs 5-HT by increasing the concentration of GDP from 0.3 to 30 and 300 mu M. Whereas dimerization of 8-OH-DPAT almost did not affect its potency at h 5-HT1A receptors (pEC(50): 7.45 and 7.40 for 8-OH-DPAT and its dimer at 30 mu M GDP), it increased efficacy at h 5-HT1A receptors. The maximal response to the 8-OH-DPAT dimer was systematically greater than the response to 8-OH-DPAT and identical to that to 5-HT; moreover in contrast to the 8-OH-DPAT monomer, the maximal response to the dimer was unaffected by increasing the GDP concentration. An enhanced [S-35]GTP gamma S binding response (44 to 63% vs 8-OH-DPAT) was also observed in the hippocampus, lateral septum, dorsal raphe and cingulate cortex of guinea-pig brain sections using autoradiography of 5-HT1A receptor-activated G-proteins. Hence, the8-OH-DPAT dimer shows increased efficacy at 5-HT1A receptors comparedto 8-OH-DPAT. The differential regulation of the maximal agonist responses by GDP suggests that the [S-35]GTP gamma S binding responses to these two ligands could be mediated by different G-protein subtypes upon activation of the 5-HT1A receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 09:11:24