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Titolo:
Low affinity use-dependent NMDA receptor antagonists show promise for clinical development
Autore:
Palmer, GC; Widzowski, D;
Indirizzi:
AstraZeneca R&D Boston, Worcester, MA 01605 USA AstraZeneca R&D Boston Worcester MA USA 01605 on, Worcester, MA 01605 USA
Titolo Testata:
AMINO ACIDS
fascicolo: 1, volume: 19, anno: 2000,
pagine: 151 - 155
SICI:
0939-4451(2000)19:1<151:LAUNRA>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
PHARMACOLOGY; KINETICS; BLOCK;
Keywords:
amino acids; NMDA; low affinity use-dependent antagonists; clinical status; epilepsy; stroke; head trauma; neurodegeneration;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
10
Recensione:
Indirizzi per estratti:
Indirizzo: Palmer, GC AstraZeneca R&D Boston, 3 Biotech,1 Innovat Dr, Worcester, MA 01605 USA AstraZeneca R&D Boston 3 Biotech,1 Innovat Dr Worcester MA USA 01605
Citazione:
G.C. Palmer e D. Widzowski, "Low affinity use-dependent NMDA receptor antagonists show promise for clinical development", AMINO ACIDS, 19(1), 2000, pp. 151-155

Abstract

The success of the low affinity use-dependent NMDA receptor. antagonists to reach clinical trials can be readily attributed to their wider margins ofsafety and lack of neurotoxicity at higher doses. Several mechanistic differences distinguish the low affinity from the high affinity use-dependent antagonists: 1) Differential regional affinities for the various NMDA receptor subtypes; 2) The static receptor blockade due to the faster on/off rate receptor kinetics which limit, but do not totally prevent the amount of Ca+2 entry into the cell during glutamate-induced depolarization; and 3) Rapidegress of the compounds from the ion channel during recovery resulting in less membrane trapping between transmission pulses. Advanced clinical trials are in progress for the following indications: epilepsy, stroke, head trauma, tardive dyskinesia, pain plus Parkinson's, Huntington's and Alzheimer's diseases.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 20:30:30