Interaction Between Allopregnanolone and Amiloride Binding Sites on the GABAA Receptor

Allopregnanolone (Allo) is a positive allosteric modulator of the GABAA receptor, and amiloride (Ami) is a competitive antagonist of the GABAA receptor. The purpose of this work was to study the combined effect of Allo and Ami on functional activity of GABAA receptor. The GABA-induced chloride curre...

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Bibliographic Details
Published in:Cell biochemistry and biophysics 2024-12
Main Authors: Bukanova, Julia V., Kondratenko, Rodion V., Solntseva, Elena I.
Format: Article
Language:English
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Summary:Allopregnanolone (Allo) is a positive allosteric modulator of the GABAA receptor, and amiloride (Ami) is a competitive antagonist of the GABAA receptor. The purpose of this work was to study the combined effect of Allo and Ami on functional activity of GABAA receptor. The GABA-induced chloride current (IGABA) was measured in isolated Purkinje cells of rat cerebellum using the patch-clamp technique and a system of fast application. Our results indicate that Allo suppresses the inhibitory effect of Ami on IGABA, the IC50 value of Ami concentration-response curve was increased from 164 to 547 µM (P 
ISSN:1085-9195
1559-0283
1559-0283
DOI:10.1007/s12013-024-01654-6