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Titolo:
5-HT1B RECEPTOR ANTAGONIST PROPERTIES OF NOVEL ARYLPIPERAZIDE DERIVATIVES OF 1-NAPHTHYLPIPERAZINE
Autore:
JORANDLEBRUN C; PAUWELS PJ; PALMIER C; MORET C; CHOPIN P; PEREZ M; MARIEN M; HALAZY S;
Indirizzi:
CTR RECH PIERRE FABRE,DIV MED CHEM,17 AVE JEAN MOULIN F-81106 CASTRESFRANCE CTR RECH PIERRE FABRE,DIV MED CHEM F-81106 CASTRES FRANCE CTR RECH PIERRE FABRE,DEPT CELLULAR & MOL BIOL F-81106 CASTRES FRANCE CTR RECH PIERRE FABRE,NEUROBIOL DIV 1 F-81106 CASTRES FRANCE
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 24, volume: 40, anno: 1997,
pagine: 3974 - 3978
SICI:
0022-2623(1997)40:24<3974:5RAPON>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG; SEROTONIN; AGONISTS; POTENT; HYPOTHERMIA; BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
C. Jorandlebrun et al., "5-HT1B RECEPTOR ANTAGONIST PROPERTIES OF NOVEL ARYLPIPERAZIDE DERIVATIVES OF 1-NAPHTHYLPIPERAZINE", Journal of medicinal chemistry, 40(24), 1997, pp. 3974-3978

Abstract

A new series of arylpiperazide derivatives of 1-naphthylpiperazine ofgeneral formula 4 has been prepared and evaluated as 5-HT1B antagonists. Binding experiments at cloned human 5-HT1A, 5-HT1B, and 5-HT1D receptors show that these derivatives are potent and selective ligands for 5-HT1B/1D subtypes with increased binding selectivity versus the 5-HT1A receptor when compared to 1-naphthylpiperazine (1-NP). Studies of inhibition of the forskolin-stimulated cAMP formation mediated by the human 5-HT1B receptor demonstrate that the nature of the arylpiperazide substituent modulates the intrinsic activity ofthese 1-NP derivatives. Among them, alen-2-yl]oxy]-1-(4-o-tolylpiperazin-1-yl)ethanone (4a)was identified as a potent neutral 5-HT1B antagonist able to antagonize the inhibition of 5-HT release induced by 5-CT (5-carbamoyltryptamine) in guinea pig hypothalamus slices. Moreover, 4a was found to potently antagonize the hypothermia induced by a selective 5-HT1B/1D agonist in vivo in the guinea pig following oral administration (ED50 = 0.13mg/kg).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 07:28:04