Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Effect of flumazenil on GABAA receptors in isolated rat hippocampal neurons.

Literature DB >> 12515312

Effect of flumazenil on GABAA receptors in isolated rat hippocampal neurons.

Michel Weiss¹, Denis Tikhonov, Svetlana Buldakova.

Abstract

Using whole cell patch-clamp recordings from pyramidal cells acutely dissociated from rat hippocampal slices, Ro-15 1788 (flumazenil, FLU) was shown to enhance the GABAA-receptor mediated currents evoked by application of gamma-aminobutyric acid (GABA) and to antagonize the enhancing effect of the benzodiazepine agonist flurazepam (FZP) on the GABAA response. Both FLU and FZP increased the peak and the steady-state components of the responses and accelerated the current decay. This suggests that both agents act via a common mechanism on GABA transmission. It is concluded that FLU possesses high affinity for the binding site, but low efficacy on the GABAA-benzodiazepine receptor. This suggests that FLU acts as a partial agonist on GABAA receptors.

Entities: Chemical Species

Mesh：

Substances：

Year: 2002 PMID： 12515312 DOI： 10.1023/a:1021674708556

Source DB: PubMed Journal: Neurochem Res ISSN： 0364-3190 Impact factor: 3.996

31 in total

Review 1. International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function.

Authors: E A Barnard; P Skolnick; R W Olsen; H Mohler; W Sieghart; G Biggio; C Braestrup; A N Bateson; S Z Langer
Journal: Pharmacol Rev Date: 1998-06 Impact factor: 25.468

Review 2. The benzodiazepine binding site of GABAA receptors.

Authors: E Sigel; A Buhr
Journal: Trends Pharmacol Sci Date: 1997-11 Impact factor: 14.819

3. A simple perfusion system for patch-clamp studies.

Authors: V S Vorobjev; I N Sharonova; H L Haas
Journal: J Neurosci Methods Date: 1996-10 Impact factor: 2.390

4. Electrophysiological evidence for agonist properties of flumazenil, a benzodiazepine receptor antagonist, in rat hippocampus slices.

Authors: S Buldakova; M Weiss
Journal: J Neurol Sci Date: 1997-08 Impact factor: 3.181

5. Reduction of inhibition by a benzodiazepine antagonist, Ro15-1788, in the rat hippocampal slice.

Authors: G L King; J J Knox; R Dingledine
Journal: Neuroscience Date: 1985-06 Impact factor: 3.590

6. Functional GABAA receptor heterogeneity of acutely dissociated hippocampal CA1 pyramidal cells.

Authors: E I Tietz; J Kapur; R L Macdonald
Journal: J Neurophysiol Date: 1999-04 Impact factor: 2.714

Review 7. Drug interactions at the GABA receptor-ionophore complex.

Authors: R W Olsen
Journal: Annu Rev Pharmacol Toxicol Date: 1982 Impact factor: 13.820

8. Benzodiazepine antagonists reduce epileptiform discharges in rat hippocampal slices.

Authors: P Polc; S S Jahromi; G Facciponte; M R Pelletier; L Zhang; P L Carlen
Journal: Epilepsia Date: 1996-10 Impact factor: 5.864

9. Benzodiazepine Ro 15-1788: electrophysiological evidence for partial agonist activity.

Authors: J H Skerritt; R L Macdonald
Journal: Neurosci Lett Date: 1983-12-30 Impact factor: 3.046

10. Selective antagonists of benzodiazepines.

Authors: W Hunkeler; H Möhler; L Pieri; P Polc; E P Bonetti; R Cumin; R Schaffner; W Haefely
Journal: Nature Date: 1981-04-09 Impact factor: 49.962

10 in total

1. Stress sensitization of ethanol withdrawal-induced reduction in social interaction: inhibition by CRF-1 and benzodiazepine receptor antagonists and a 5-HT1A-receptor agonist.

Authors: George R Breese; Darin J Knapp; David H Overstreet
Journal: Neuropsychopharmacology Date: 2004-03 Impact factor: 7.853

2. Analysis of the excitatory and inhibitory components of postsynaptic currents recorded in pyramidal neurons and interneurons in the rat hippocampus.

Authors: S L Buldakova; D B Tikhonov; L G Magazanik
Journal: Neurosci Behav Physiol Date: 2005-10

3. Modulation of ethanol withdrawal-induced anxiety-like behavior during later withdrawals by treatment of early withdrawals with benzodiazepine/gamma-aminobutyric acid ligands.

Authors: Darin J Knapp; David H Overstreet; George R Breese
Journal: Alcohol Clin Exp Res Date: 2005-04 Impact factor: 3.455

4. The dual modulatory effects of efavirenz on GABA_A receptors are mediated via two distinct sites.

Authors: Renqi Huang; Zhenglan Chen; Sean Dolan; John A Schetz; Glenn H Dillon
Journal: Neuropharmacology Date: 2017-04-27 Impact factor: 5.250

5. Behavioral effects of flumazenil in the social conflict test in mice.

Authors: L Uhlírová; M Sustková-Fiserová; M Krsiak
Journal: Psychopharmacology (Berl) Date: 2003-09-05 Impact factor: 4.530

6. Discriminative stimulus effects of L-838,417 (7-tert-butyl-3-(2,5-difluoro-phenyl)-6-(2-methyl-2H-[1,2,4]triazol-3-ylmethoxy)-[1,2,4]triazolo[4,3-b]pyridazine): role of GABA(A) receptor subtypes.

Authors: Stephanie C Licata; Donna M Platt; Daniela Rüedi-Bettschen; John R Atack; Gerard R Dawson; Michael L Van Linn; James M Cook; James K Rowlett
Journal: Neuropharmacology Date: 2009-10-22 Impact factor: 5.250

Review 7. Pharmacological Modulation of GABA Function in Autism Spectrum Disorders: A Systematic Review of Human Studies.

Authors: Natascia Brondino; Laura Fusar-Poli; Cristina Panisi; Stefano Damiani; Francesco Barale; Pierluigi Politi
Journal: J Autism Dev Disord Date: 2016-03