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Titolo:
ORPHENADRINE IS AN UNCOMPETITIVE N-METHYL-D-ASPARTATE (NMDA) RECEPTORANTAGONIST - BINDING AND PATCH-CLAMP STUDIES
Autore:
KORNHUBER J; PARSONS CG; HARTMANN S; RETZ W; KAMOLZ S; THOME J; RIEDERER P;
Indirizzi:
UNIV WURZBURG,DEPT PSYCHIAT,FUCHSLEINSTR 15 D-97080 WURZBURG GERMANY MERCK & CO INC,DEPT PHARMACOL FRANKFURT GERMANY
Titolo Testata:
Journal of neural transmission
fascicolo: 3, volume: 102, anno: 1995,
pagine: 237 - 246
SICI:
0300-9564(1995)102:3<237:OIAUN(>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTIPARKINSONIAN DRUGS; BASAL GANGLIA; AMANTADINE; ACETYLCHOLINE; PARKINSONISM; MEMANTINE; SYSTEMS; CHANNEL; RELEASE; BRAIN;
Keywords:
UNCOMPETITIVE N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST; NMDA; ORPHENADRINE; PATCH CLAMP; SUPERIOR COLLICULUS CULTURE; [H-3] MK-801 BINDING; CORTICAL MEMBRANES; GLUTAMATE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
J. Kornhuber et al., "ORPHENADRINE IS AN UNCOMPETITIVE N-METHYL-D-ASPARTATE (NMDA) RECEPTORANTAGONIST - BINDING AND PATCH-CLAMP STUDIES", Journal of neural transmission, 102(3), 1995, pp. 237-246

Abstract

Orphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug for many years. Here we show that orphenadrine inhibits [H-3]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cortex with a K-i-value of 6.0 +/- 0.7 mu M. The NMDA receptor antagonistic effects of orphenadrine were assessed using concentration-and patch-clamp techniques on cultured superior colliculus neurones. Orphenadrine blocked open NMDA receptor channels with fast kinetics and in a strongly voltage-dependent manner. The IC50-value against steady state currents at -70 mV was 16.2 +/- 1.6 mu M (n = 6). Orphenadrineexhibited relatively fast, concentration-dependent open channel blocking kinetics (K-on 0.013 +/- 0.002 10(6) M(-1) S-1) whereas the offsetrate was concentration-independent (K-off 0.230 +/- 0.004 S-1). Calculation of the ratio K-off/K-on revealed an apparent K-d-value of 17.2 mu M which is nearly identical to the IC50 calculated at equilibrium.

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Documento generato il 12/07/20 alle ore 13:21:45