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Titolo:
BUDIPINE IS A LOW-AFFINITY, N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST - PATCH-CLAMP STUDIES IN CULTURED STRIATAL, HIPPOCAMPAL, CORTICAL AND SUPERIOR COLLICULUS NEURONS
Autore:
PARSONS CG; HARTMANN S; SPIELMANNS P;
Indirizzi:
MERZ & CO,DEPT PHARMACOL,ECKENHEIMER LANDSTR 100-104 D-60318 FRANKFURT GERMANY
Titolo Testata:
Neuropharmacology
fascicolo: 6, volume: 37, anno: 1998,
pagine: 719 - 727
SICI:
0028-3908(1998)37:6<719:BIALNR>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTIPARKINSONIAN DRUG BUDIPINE; NMDA RECEPTORS; PARKINSONS-DISEASE; CHANNEL BLOCKERS; RAT HIPPOCAMPAL; BASAL GANGLIA; MEMANTINE; AMANTADINE; KINETICS; RELEASE;
Keywords:
AMANTADINE; BUDIPINE; CORTICAL AND HIPPOCAMPAL CULTURES; MEMANTINE; PATCH CLAMP; STRIATAL; UNCOMPETITIVE N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
C.G. Parsons et al., "BUDIPINE IS A LOW-AFFINITY, N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST - PATCH-CLAMP STUDIES IN CULTURED STRIATAL, HIPPOCAMPAL, CORTICAL AND SUPERIOR COLLICULUS NEURONS", Neuropharmacology, 37(6), 1998, pp. 719-727

Abstract

The NMDA receptor antagonistic effects of budipine were assessed using concentration- and patch-clamp techniques on cultured striatal: hippocampal, cortical and superior colliculus neurones. Inward current responses of striatal neurones to NMDA (200 mu M) at - 70 mV were antagonized by budipine in a concentration-dependent manner (50% inhibitory concentration (IC50) 59.4 +/- 10.7 mu M, n = 17) with 24 times lower potency than memantine but similar potency to amantadine. In striatal neurones, budipine blocked outward currents at + 70 mV with an IC50 of 827 mu M, suggesting that the binding site is less deep in the channel (delta = 0.45) than for memantine. However, more detailed analysis of the fractional block by budipine 300 mu M in hippocampal neurones gavea delta-value of 0.90, but revealed that 28% block is mediated at a voltage-independent site. This voltage-insensitive site was accessible in the absence of agonist. Budipine exhibited concentration-dependent open channel blocking kinetics (kappa(on) = 0.7110(4) M-1 s(-1)) whereas the fast offset rate was concentration-independent (kappa(off) = 0.63 s(-1)). Calculation of the ratio kappa(off)/kappa(on) revealed an apparent K-d value of 88.7 mu M. Budipine, memantine and amantadine had similar effects against NMDA-induced currents in cultured hippocampal: cortical and superior colliculus neurones, although amantadine was somewhat more potent in cultured striatal neurones. The relevance of NMDA receptor antagonism to the anti-Parkinsonian effects of budipine remains to be established. (C) 1998 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 15:03:13