Modulation of GABA-A receptors of astrocytes and STC-1 cells by taurine structural analogs

Reyes-Haro, Daniel, Cabrera-Ruíz, Elizabeth, Estrada-Mondragón, Argel, Miledi, Ricardo and Martínez-Torres, Ataúlfo (2014) Modulation of GABA-A receptors of astrocytes and STC-1 cells by taurine structural analogs. Amino Acids, 46 11: 2587-2593. doi:10.1007/s00726-014-1813-0

Author Reyes-Haro, Daniel
Cabrera-Ruíz, Elizabeth
Estrada-Mondragón, Argel
Miledi, Ricardo
Martínez-Torres, Ataúlfo
Title Modulation of GABA-A receptors of astrocytes and STC-1 cells by taurine structural analogs
Journal name Amino Acids   Check publisher's open access policy
ISSN 0939-4451
Publication date 2014-08-15
Sub-type Article (original research)
DOI 10.1007/s00726-014-1813-0
Open Access Status Not yet assessed
Volume 46
Issue 11
Start page 2587
End page 2593
Total pages 7
Place of publication Wien, Austria
Publisher Springer
Language eng
Abstract Taurine activates and modulates GABA receptors in vivo as well as those expressed in heterologous systems. This study aimed to determine whether the structural analogs of taurine: homotaurine and hypotaurine, have the ability to activate GABA-A receptors that include GABAρ subunits. The expression of GABA-A receptors containing GABAρ has been reported in the STC-1 cells and astrocytes. In both cell types, taurine, homo-, and hypotaurine gated with low efficiency a picrotoxin-sensitive GABA-A receptor. The known bimodal modulatory effect of taurine on GABAρ receptors was not observed; however, differences between the activation and deactivation rates were detected when they were perfused together with GABA. In silico docking simulations suggested that taurine, hypo-, and homotaurine do not form a cation-π interaction such as that generated by GABA in the agonist-binding site of GABAρ. This observation complements the electrophysiological data suggesting that taurine and its analogs act as partial agonists of GABA-A receptors. All the observations above suggest that the structural analogs of taurine are partial agonists of GABA-A receptors that occupy the agonist-binding site, but their structures do not allow the proper interaction with the receptor to fully gate its Cl- channel.
Keyword Astrocytes
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ
Additional Notes Published online: 15 August 2014.

Document type: Journal Article
Sub-type: Article (original research)
Collections: Non HERDC
Queensland Brain Institute Publications
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Created: Thu, 04 Sep 2014, 19:54:11 EST by Argel Estrada on behalf of Queensland Brain Institute