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Titolo:
Inhibitors of AMPA and kainate receptors
Autore:
Madsen, U; Stensbol, TB; Krogsgaard-Larsen, P;
Indirizzi:
Royal Danish Sch Pharm, Dept Med Chem, DK-2100 Copenhagen, Denmark Royal Danish Sch Pharm Copenhagen Denmark DK-2100 00 Copenhagen, Denmark
Titolo Testata:
CURRENT MEDICINAL CHEMISTRY
fascicolo: 11, volume: 8, anno: 2001,
pagine: 1291 - 1301
SICI:
0929-8673(200109)8:11<1291:IOAAKR>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMINO-ACID RECEPTORS; NON-NMDA ANTAGONISTS; METHYL-D-ASPARTATE; CENTRAL-NERVOUS-SYSTEM; CHANNEL BLOCKING DRUG; HIGH-AFFINITY LIGAND; GLUTAMATE-RECEPTOR; ANTICONVULSANT ACTIVITY; RAT-BRAIN; ABSOLUTE STEREOCHEMISTRY;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
136
Recensione:
Indirizzi per estratti:
Indirizzo: Madsen, U Royal Danish Sch Pharm, Dept Med Chem, Universitetsparken 2, DK-2100 Copenhagen, Denmark Royal Danish Sch Pharm Universitetsparken 2 Copenhagen Denmark DK-2100
Citazione:
U. Madsen et al., "Inhibitors of AMPA and kainate receptors", CURR MED CH, 8(11), 2001, pp. 1291-1301

Abstract

The glutamate receptor system is implicated in the development and maintenance of epileptic seizures, and animal studies have disclosed potent anticonvulsant activity of a number of inhibitors of AMPA and/or kainate (KA) receptor activity. These results make such inhibitors potential future antiepileptic drugs. Different series of compounds with inhibitory activity towards AMPA receptors have been developed. Most of these inhibitors are structurally derived from AMPA, quinoxalinedione or 2,3-benzodiazepine. In contrast, only a limited number of inhibitors of KA receptor activity have been developed, most of which contain quinoxalinedione or decahydroisoquinoline skeletons. In spite of promising anticonvulsant activity in various animal model studies, no AMPA/KA receptor inhibitors are in clinical use against epilepsy today. Based on molecular biology studies, AMPA and KA receptors are at present divided into four and five subtypes, respectively, and attempts to develop subtype selective compounds have been initiated. Future studies and development of such compounds will indicate whether AMPA/KA receptor inhibition is a feasible therapeutic strategy for the treatment of epilepsy.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 07:28:22