Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
SYNTHESIS, BINDING-AFFINITY AND INTRINSIC ACTIVITY OF NEW ANILIDE DERIVATIVES OF SEROTONIN AT HUMAN 5-HT1D RECEPTORS
Autore:
PEREZ M; AYERBE N; FOURRIER C; SIGOGNEAU I; PAUWELS PJ; PALMIER C; JOHN GW; VALENTIN JP; HALAZY S;
Indirizzi:
CTR RECH PIERRE FABRE,DIV MED CHEM,17 AVE JEAN MOULIN F-81106 CASTRESFRANCE CTR RECH PIERRE FABRE,CELLULAR & MOL NEUROBIOL LAB F-81106 CASTRES FRANCE CTR RECH PIERRE FABRE,DIV CARDIOVASC DIS F-81106 CASTRES FRANCE
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 2, volume: 32, anno: 1997,
pagine: 129 - 134
SICI:
0223-5234(1997)32:2<129:SBAIAO>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
BOVINE CEREBRAL-ARTERIES; POTENT AGONISTS; SUMATRIPTAN; CLASSIFICATION; PHARMACOLOGY; MIGRAINE; ANALOGS;
Keywords:
ANILIDE; 5-HT1D RECEPTOR AGONIST; SEROTONIN; MIGRAINE; SUMATRIPTAN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
23
Recensione:
Indirizzi per estratti:
Citazione:
M. Perez et al., "SYNTHESIS, BINDING-AFFINITY AND INTRINSIC ACTIVITY OF NEW ANILIDE DERIVATIVES OF SEROTONIN AT HUMAN 5-HT1D RECEPTORS", European journal of medicinal chemistry, 32(2), 1997, pp. 129-134

Abstract

The design and synthesis of a new series of anilide derivatives of serotonin is described. Binding affinity and intrinsic activity were evaluated at cloned human 5-HT1D alpha, 5-HT1D beta and 5-HT1A receptors. Modification of the terminal substituent on the aromatic moiety (R(1)) was investigated and optimal affinity, activity and selectivity for 5-HT1D versus 5-HT1A receptors were obtained for the sulfonamide derivatives 9 and 10. Functional activity was also assessed in the New Zealand white rabbit saphenous vein contraction model, in which most of the compounds behaved as full agonists. Further structural modificationsare also described, eg, replacement of the oxygen for carbon atom at the 5-position of the tryptamine moiety or terminal N-dimethylation.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 10:22:46