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Titolo:
SYNTHESES OF O-METHYLASPARVENONE-DERIVED SEROTONIN-RECEPTOR ANTAGONISTS
Autore:
BOS M; STADLER H; WICHMANN J; JENCK F; MARTIN JR; MOREAU JL; SLEIGHT AJ;
Indirizzi:
F HOFFMANN LA ROCHE & CO LTD,DIV PHARMA,PRECLIN CNS RES CH-4070 BASELSWITZERLAND
Titolo Testata:
Helvetica Chimica Acta
fascicolo: 3, volume: 81, anno: 1998,
pagine: 525 - 538
SICI:
0018-019X(1998)81:3<525:SOOSA>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
M. Bos et al., "SYNTHESES OF O-METHYLASPARVENONE-DERIVED SEROTONIN-RECEPTOR ANTAGONISTS", Helvetica Chimica Acta, 81(3), 1998, pp. 525-538

Abstract

Based on O-methylasparvenone (I), a N-free 5HT(2C) antagonist with moderate affinity (pK(i) = 6.7), derivatives bearing dimethylamino (7), (dimethylamino)methyl (17, 18, 21, and 22), and aminomethyl substituents (26) in place of the benzylic OH group of 1 as well as pyrrolidine-(33) and piperidine-fused derivatives (29, 43, and 45) were synthesized. In contrast to the lead structure 1, these new ligands were activein vivo in the rat. The tricycles 33 and 45 display high affinities for the 5HT(2C) receptor (pK(i) = 8).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:36:36