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Titolo:
LCARBAMOYL)-1,2,3,5-TETRAHYDROPYRROLO[2,3-F]INDOLE - A NOVEL 5-HT2C 5-HT2B RECEPTOR ANTAGONIST WITH IMPROVED AFFINITY, SELECTIVITY, AND ORAL ACTIVITY
Autore:
FORBES IT; HAM P; BOOTH DH; MARTIN RT; THOMPSON M; BAXTER GS; BLACKBURN TP; GLEN A; KENNETT GA; WOOD MD;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,DISCOVERY RES,DEPT MED CHEM,NEW FRONTIERS SCI PK,3RD AVE HARLOW CM19 5AW ESSEX ENGLAND SMITHKLINE BEECHAM PHARMACEUT,DISCOVERY RES,DEPT PSYCHIAT RES HARLOW CM19 5AW ESSEX ENGLAND SMITHKLINE BEECHAM PHARMACEUT,DISCOVERY RES,DEPT NEUROL RES HARLOW CM19 5AW ESSEX ENGLAND
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 14, volume: 38, anno: 1995,
pagine: 2524 - 2530
SICI:
0022-2623(1995)38:14<2524:L-AN55>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; CHOROID-PLEXUS; 5-HYDROXYTRYPTAMINE2F; CLONING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
I.T. Forbes et al., "LCARBAMOYL)-1,2,3,5-TETRAHYDROPYRROLO[2,3-F]INDOLE - A NOVEL 5-HT2C 5-HT2B RECEPTOR ANTAGONIST WITH IMPROVED AFFINITY, SELECTIVITY, AND ORAL ACTIVITY", Journal of medicinal chemistry, 38(14), 1995, pp. 2524-2530

Abstract

The preparation of a series of conformationally restricted analogues of indolylurea 1, namely tetrahydropyrroloindoles and tetrahydropyrroloquinolines, is described. The binding affinities of these compounds at 5-HT2A, 5-HT2B, and 5-HT2C receptors were determined. Of these compounds, the 1,2,3,5-tetrahydropyrrolo[2,3-f]indole derivative, compound 11, was found to have high affinity for the 5-HT2C (pK(I) 8.0) and 5-HT2B receptors (pA(2) 8.5), with excellent selectivity over the 5-HT2A and various other receptors (pK(I) <6). 11 is also considerably more active than 1 in both an in vitro functional model, 5-HT-stimulated phosphoinositol hydrolysis (pK(B) 8.8), and an in vivo functional model, mCPP-induced hypolocomotion (ID50 5.5 mg/kg po). 11 should therefore be of significant utility as a pharmacological tool to delineate the functional significance of blockade of 5-HT2B and 5-HT2C receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 19:16:39