Differential modulation of the GYKI 53784-induced inhibition of AMPA currents by various AMPA-positive modulators in cerebellar Purkinje cells

详细信息    查看全文

• 作者：Kapus ; Gá ; bor ; Bó ; di ; Ilona ; et. al.
• 关键词：AMPA receptor ; Purkinje cell ; GYKI 53784 ; Aniracetam ; Cyclothiazide ; 1-BCP ; BDP-12
• 刊名：European Journal of Pharmacology
• 出版年：2000
• 出版时间：May 26, 2000
• 年：2000
• 卷：397
• 期：1
• 页码：43-47
• 全文大小：101 K

文摘

The effects of various (S)-α-amino-3-hydroxy-5-methyl-4-izoxazole-propionate (AMPA) receptor modulators on AMPA-induced whole-cell currents were compared in isolated rat cerebellar Purkinje cells. The positive modulators, aniracetam, cyclothiazide, 1-(1,3-benzodioxol-5-ylcarbonyl)-piperidine (1-BCP), and 1-(quinoxaline-6-ylcarbonyl)-piperidine (BDP-12), dose-dependently potentiated the steady-state component of AMPA currents. The negative modulator, (−)1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3-methylcarbamoyl-2,3-benzodiazepine (GYKI 53784), dose-dependently suppressed AMPA responses. Its concentration–response curve was shifted to the right in a parallel fashion by all positive modulators, indicating a competitive type of interaction. However, the relative potencies of the positive modulators were different with regard to the enhancement of AMPA responses and the reversal of GYKI 53784-induced inhibition, respectively. It is supposed that positive modulators act at multiple allosteric sites and that they interact with GYKI 53784 at only one of these sites. Publisher: Elsevier Science Language of Publication: English Item Identifier: S0014-2999(00)00302-2 Publication Type: Miscellaneous ISSN: 0014-2999 Cited by:

1. Gates, M.; Ogden, A.; Bleakman, D.,""Pharmacological effects of AMPA receptor potentiators LY392098 and LY404187 on rat neuronal AMPA receptors in vitro""Neuropharmacology2001pp. 984-991
   Bibliographic PageFull Text
2. Linden, Anni-Maija; Yu, Hong; Zarrinmayeh, Hamideh; Wheeler, William J.; Skolnick, Phil,""Binding of an AMPA receptor potentiator ([³H]LY395153) to native and recombinant AMPA receptors³""Neuropharmacology2001pp. 1010-1018
   Bibliographic PageFull Text
3. Gabryel, Bozena; Adamczyk, Jakub; Huzarska, Malgorzata; Pudelko, Anna; Trzeciak, Henryk I.,""Aniracetam Attenuates Apoptosis of Astrocytes Subjected to Simulated Ischemia In Vitro""Neurotoxicology2002pp. 385-395
   Bibliographic PageFull Text
4. Stone, Trevor W.; Addae, Jonas I.,""The pharmacological manipulation of glutamate receptors and neuroprotection""European Journal of Pharmacology2002pp. 285-296
   Bibliographic PageFull Text
5. Fischer, Wolfgang; Franke, Heike; Scheibler, Peter; Allgaier, Clemens; Illes, Peter,""AMPA-induced Ca²⁺ influx in cultured rat cortical nonpyramidal neurones: pharmacological characterization using fura-2 microfluorimetry""European Journal of Pharmacology2002pp. 53-62
   Bibliographic PageFull Text
6. Ghersi, Chiara; Bonfanti, Andrea; Manzari, Benedetta; Feligioni, Marco; Raiteri, Maurizio; Pittaluga, Anna,""Pharmacological heterogeneity of release-regulating presynaptic AMPA/kainate receptors in the rat brain: study with receptor antagonists""Neurochemistry International2003pp. 283-292
   Bibliographic PageFull Text

---

Footnotes:

1. Present address: College of Medicine Institute of Molecular Pharmacology and Biophysics, University of Cincinnati Medical Center, P.O. Box 670828, Cincinnati OH 45267-0828, USA.

2. Present address: Gedeon Richter Chemical Works Ltd., P.O. Box 27, H-1475 Budapest, Hungary.

3. The first two authors contributed equally to this work.