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Titolo:
Opening of neuronal K+ channels by flupirtine
Autore:
Kornhuber, J; Maler, M; Wiltfang, J; Bleich, S; Degner, D; Ruther, E;
Indirizzi:
Univ Gottingen, Psychiat Klin, D-3400 Gottingen, Germany Univ Gottingen Gottingen Germany D-3400 Klin, D-3400 Gottingen, Germany
Titolo Testata:
FORTSCHRITTE DER NEUROLOGIE PSYCHIATRIE
fascicolo: 10, volume: 67, anno: 1999,
pagine: 466 - 475
SICI:
0720-4299(199910)67:10<466:OONKCB>2.0.ZU;2-6
Fonte:
ISI
Lingua:
GER
Soggetto:
METHYL-D-ASPARTATE; POTASSIUM CHANNEL; HIPPOCAMPAL-NEURONS; ANALGESIC FLUPIRTINE; SUBSTANCE-P; TRIAMINOPYRIDINE FLUPIRTINE; ANTINOCICEPTIVE ACTIVITY; MEMBRANE EXCITABILITY; EPILEPTIFORM ACTIVITY; PHYSICAL-DEPENDENCE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
84
Recensione:
Indirizzi per estratti:
Indirizzo: Kornhuber, J Univ Gottingen, Abt Psychiat, Von Siebold Str 5, D-37075 Gottingen, Germany Univ Gottingen Von Siebold Str 5 Gottingen Germany D-37075 y
Citazione:
J. Kornhuber et al., "Opening of neuronal K+ channels by flupirtine", F NEUR PSYC, 67(10), 1999, pp. 466-475

Abstract

The spectrum of action of flupirtine includes analgesic, muscle-relaxant and neuroprotective properties. The substance's mechanism of action has yet to be fully explained. Over the past few years, however, evidence has accumulated that flupirtine interacts with the glutamatergic N-Methyl-D-Aspartate (NMDA) receptor. Although it was not possible to demonstrate a direct effect an the NMDA receptor, all of the findings pointed to an indirect influence on the NMDA receptor in the sense of a functional NMDA antagonism. It was thus postulated that a site of action "up- or downstream" of the NMDA receptor is influenced. Such a site of action proved to be the G-protein-activated inwardly rectifying K+ channels (GIRK), the opening of which leads toa stabilisation of the resting membrane potential of neuronal cells and thus causes an indirect inhibition of the NMDA receptor. At therapeutically relevant concentrations, flupirtine is a neuronal potassium channel opener. This mechanism may explain the spectrum of action of flupirtine. Selective neuronal potassium channel opening (SNEPCO) thus proves to be a new principle of action, malting flupirtine the prototype of a new substance class with analgesic, muscle-relaxant and neuroprotective properties. The experimental basis for this working hypothesis and the resulting model concepts are presented from the perspective of a four-stage approach.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 14:41:31