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Titolo:
H-TETRAZOL-5-YL)DECAHYDROISOQUINOLINE-3-CARBOXYLIC ACID, A NOVEL, COMPETITIVE, SYSTEMICALLY ACTIVE NMDA AND AMPA RECEPTOR ANTAGONIST
Autore:
ORNSTEIN PL; ARNOLD MB; ALLEN NK; LEANDER JD; TIZZANO JP; LODGE D; SCHOEPP DD;
Indirizzi:
ELI LILLY & CO,LILLY CORP CTR,LILLY RES LABS,DROP CODE 0510 INDIANAPOLIS IN 46285 ELI LILLY & CO,LILLY RES CTR LTD WINDLESHAM GU20 6PH SURREY ENGLAND
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 25, volume: 38, anno: 1995,
pagine: 4885 - 4890
SICI:
0022-2623(1995)38:25<4885:HAANC>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
METHYL-D-ASPARTATE; PHENCYCLIDINE-LIKE DRUGS; BINDING; GLUCOSE; BRAIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
P.L. Ornstein et al., "H-TETRAZOL-5-YL)DECAHYDROISOQUINOLINE-3-CARBOXYLIC ACID, A NOVEL, COMPETITIVE, SYSTEMICALLY ACTIVE NMDA AND AMPA RECEPTOR ANTAGONIST", Journal of medicinal chemistry, 38(25), 1995, pp. 4885-4890

Abstract

We report the synthesis and characterization of 6 (LY246492), which is a competitive N-methyl-D-aspartate (NMDA) and amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propanoic acid (AMPA) receptor antagonist. Tetrazole-substituted amino acid 6 was prepared in four steps from the recently described aldehyde 7. The optical isomers (-)-6 and (+)-6 were obtained from the same sequence of reactions using the corresponding isomers of 7. The compound displaces both NMDA and AMPA receptor binding andantagonizes depolarizations in cortical slices evoked by both NMDA and AMPA. In mice and pigeons, the compound showed antagonism of responses mediated through NMDA and AMPA receptors. Using the resolved optical isomers of 6, both NMDA and AMPA antagonist activities were found toreside in a single isomer, (-)-6.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 01:30:08