scholarly journals The small molecule CLP257 does not modify activity of the K+–Cl− co-transporter KCC2 but does potentiate GABAA receptor activity

2017 ◽  
Vol 23 (12) ◽  
pp. 1394-1396 ◽  
Author(s):  
Ross A Cardarelli ◽  
Karen Jones ◽  
Lucie I Pisella ◽  
Heike J Wobst ◽  
Lisa J McWilliams ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Small Molecule ◽  
Receptor Activity ◽  
Modify Activity

Reply to The small molecule CLP257 does not modify activity of the K+–Cl− co-transporter KCC2 but does potentiate GABAA receptor activity

2017 ◽  
Vol 23 (12) ◽  
pp. 1396-1398 ◽  
Author(s):  
Martin Gagnon ◽  
Marc J Bergeron ◽  
Jimena Perez-Sanchez ◽  
Isabel Plasencia-Fernández ◽  
Louis-Etienne Lorenzo ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Small Molecule ◽  
Receptor Activity ◽  
Modify Activity

Synthesis and GABAA receptor activity of 6-oxa-analogs of neurosteroids

Steroids ◽  
2000 ◽  
Vol 65 (6) ◽  
pp. 349-356 ◽  
Author(s):  
Daniel Nicoletti ◽  
Alberto A Ghini ◽  
Roman Furtmüller ◽  
Werner Sieghart ◽  
Robert H Dodd ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Receptor Activity

Inflammation Increases Neuronal Sensitivity to General Anesthetics

2016 ◽  
Vol 124 (2) ◽  
pp. 417-427 ◽  
Author(s):  
Sinziana Avramescu ◽  
Dian-Shi Wang ◽  
Irene Lecker ◽  
William T. H. To ◽  
Antonello Penna ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Cortical Neurons ◽  
Receptor Activity ◽  
Aminobutyric Acid ◽  
General Anesthetics ◽  
Enhanced Sensitivity ◽  
Behavioral Sensitivity ◽  
Underlying Mechanisms

Abstract Background Critically ill patients with severe inflammation often exhibit heightened sensitivity to general anesthetics; however, the underlying mechanisms remain poorly understood. Inflammation increases the number of γ-aminobutyric acid type A (GABAA) receptors expressed on the surface of neurons, which supports the hypothesis that inflammation increases up-regulation of GABAA receptor activity by anesthetics, thereby enhancing the behavioral sensitivity to these drugs. Methods To mimic inflammation in vitro, cultured hippocampal and cortical neurons were pretreated with interleukin (IL)-1β. Whole cell patch clamp methods were used to record currents evoked by γ-aminobutyric acid (GABA) (0.5 μM) in the absence and presence of etomidate or isoflurane. To mimic inflammation in vivo, mice were treated with lipopolysaccharide, and several anesthetic-related behavioral endpoints were examined. Results IL-1β increased the amplitude of current evoked by GABA in combination with clinically relevant concentrations of either etomidate (3 μM) or isoflurane (250 μM) (n = 5 to 17, P < 0.05). Concentration–response plots for etomidate and isoflurane showed that IL-1β increased the maximal current 3.3-fold (n = 5 to 9) and 1.5-fold (n = 8 to 11), respectively (P < 0.05 for both), whereas the half-maximal effective concentrations were unchanged. Lipopolysaccharide enhanced the hypnotic properties of both etomidate and isoflurane. The immobilizing properties of etomidate, but not isoflurane, were also increased by lipopolysaccharide. Both lipopolysaccharide and etomidate impaired contextual fear memory. Conclusions These results provide proof-of-concept evidence that inflammation increases the sensitivity of neurons to general anesthetics. This increase in anesthetic up-regulation of GABAA receptor activity in vitro correlates with enhanced sensitivity for GABAA receptor–dependent behavioral endpoints in vivo.

scholarly journals Modulation of GABAA receptor activity by alphaxalone

1987 ◽  
Vol 90 (3) ◽  
pp. 491-500 ◽  
Author(s):  
Glen A. Cottrell ◽  
Jeremy J. Lambert ◽  
John A. Peters
Keyword(s):  
Gabaa Receptor ◽  
Receptor Activity

scholarly journals Distinct Modulation of Spontaneous and GABA-Evoked Gating by Flurazepam Shapes Cross-Talk Between Agonist-Free and Liganded GABAA Receptor Activity

2018 ◽  
Vol 12 ◽  
Author(s):  
Magdalena Jatczak-Śliwa ◽  
Katarzyna Terejko ◽  
Marek Brodzki ◽  
Michał A. Michałowski ◽  
Marta M. Czyzewska ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Cross Talk ◽  
Receptor Activity

scholarly journals NMDA receptor activity downregulates KCC2 resulting in depolarizing GABAA receptor–mediated currents

2011 ◽  
Vol 14 (6) ◽  
pp. 736-743 ◽  
Author(s):  
Henry H C Lee ◽  
Tarek Z Deeb ◽  
Joshua A Walker ◽  
Paul A Davies ◽  
Stephen J Moss
Keyword(s):  
Nmda Receptor ◽  
Gabaa Receptor ◽  
Receptor Activity
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