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Titolo:
THE GLYCINE SITE ON THE NMDA RECEPTOR - STRUCTURE-ACTIVITY-RELATIONSHIPS AND POSSIBLE THERAPEUTIC APPLICATIONS
Autore:
DANNHARDT G; KOHL BK;
Indirizzi:
UNIV MAINZ,INST PHARM,STAUDINGERWEG 5 D-55099 MAINZ GERMANY
Titolo Testata:
Current medicinal chemistry
fascicolo: 4, volume: 5, anno: 1998,
pagine: 253 - 263
SICI:
0929-8673(1998)5:4<253:TGSOTN>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
D-ASPARTATE RECEPTOR; CORTICAL NEURONAL MORPHOLOGY; CEREBRAL GLUCOSE-METABOLISM; PARKINSONS-DISEASE; KYNURENIC ACID; GLUTAMATE RECEPTORS; ALZHEIMERS-DISEASE; BINDING-SITE; ANTAGONISTS; MILACEMIDE;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
55
Recensione:
Indirizzi per estratti:
Citazione:
G. Dannhardt e B.K. Kohl, "THE GLYCINE SITE ON THE NMDA RECEPTOR - STRUCTURE-ACTIVITY-RELATIONSHIPS AND POSSIBLE THERAPEUTIC APPLICATIONS", Current medicinal chemistry, 5(4), 1998, pp. 253-263

Abstract

L-glutamate is the most important fast excitatory neurotransmitter inthe mammalian central nervous system. Glutamate receptors are classified into two main categories: ionotropic and metabotropic. The N-methyl-D-aspartate (NMDA) receptor, which is associated with an ion channel, seems to play an important role in glutamate excitotoxicity, a process thought to be involved in a number of neurodegenerative disorders such as focal cerebral ischaemia (stroke), Parkinsonis, Huntingtonis, Alzheimeris disease, schizophrenia and epilepsy. The unique glycine site on the NMDA receptor, discovered by Johnson and Ascher in 1987, represents an interesting target for the development of neuroprotectve compounds. Glycine antagonists may offer advantages over other NMDA antagonists in terms of their side-effect profile, especially in the long-term treatment of chronical neurodegenerative disorders but also in thetreatment of serious medical emergencies with a significant morbidityand mortality like status epilepticus or stroke. So far it is not clear whether NMDA receptor antagonists including glycine antagonists would be suitable for chronic administration because of their effects on cognition, learning and motor function. High-affinity, in vivo potent,glycine antagonists of great structural diversity (i. e. pyrido[2,3-b]pyrazine-N-oxides, indole-2-carboxylates, 4-substituted-3-phenylquinoline-2(1H)-ones and alkyl-substituted 1,4-dihydro-quinoxaline-2,3-diones) are now available and their suitability for long-term treatment ofchronical neurodegenerative disorders has to be investigated in clinical trials.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 08:48:39