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Titolo:
NOVEL AGONISTS OF 5HT(2C) RECEPTORS - SYNTHESIS AND BIOLOGICAL EVALUATION OF SUBSTITUTED 2-(INDOL-1-YL)-1-METHYLETHYLAMINES AND 2-(INDENO[1,2-B]PYRROL-1-YL)-1-METHYLETHYLAMINES - IMPROVED THERAPEUTICS FOR OBSESSIVE-COMPULSIVE DISORDER
Autore:
BOS M; JENCK F; MARTIN JR; MOREAU JL; SLEIGHT AJ; WICHMANN J; WIDMER U;
Indirizzi:
F HOFFMANN LA ROCHE & CO LTD,PRECLIN CNS RES,DIV PHARMA CH-4070 BASELSWITZERLAND
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 17, volume: 40, anno: 1997,
pagine: 2762 - 2769
SICI:
0022-2623(1997)40:17<2762:NAO5R->2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
RATS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
M. Bos et al., "NOVEL AGONISTS OF 5HT(2C) RECEPTORS - SYNTHESIS AND BIOLOGICAL EVALUATION OF SUBSTITUTED 2-(INDOL-1-YL)-1-METHYLETHYLAMINES AND 2-(INDENO[1,2-B]PYRROL-1-YL)-1-METHYLETHYLAMINES - IMPROVED THERAPEUTICS FOR OBSESSIVE-COMPULSIVE DISORDER", Journal of medicinal chemistry, 40(17), 1997, pp. 2762-2769

Abstract

The syntheses of a series of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines are reported. The binding affinities of the compounds at 5HT(2C) and 5HT(2A) receptors (79% homology in the transmembrane domain) were determined. Theligands displayed selectivity for 5HT(2C) receptors relative to 5HT(2A) receptors. Compounds were functionally characterized both in vitro and in vivo as 5HT(2C) receptor agonists. 5f, 5l, 5n, 5o, 5q, 14c, 14f, 14k, and 14m exhibited anticompulsive activity in an animal model ofobsessive compulsive disorder.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/01/20 alle ore 07:19:26