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Differential modulation of human GABAC-ρ1 receptor by sulfur-containing compounds structurally related to taurine

Overview of attention for article published in BMC Neuroscience, August 2018
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Title
Differential modulation of human GABAC-ρ1 receptor by sulfur-containing compounds structurally related to taurine
Published in
BMC Neuroscience, August 2018
DOI 10.1186/s12868-018-0448-6
Pubmed ID
Authors

Lenin David Ochoa-de la Paz, Martin González-Andrade, Herminia Pasantes-Morales, Rodrigo Franco, Rubén Zamora-Alvarado, Edgar Zenteno, Hugo Quiroz-Mercado, Roberto Gonzales-Salinas, Rosario Gulias-Cañizo

Abstract

The amino acid taurine (2-Aminoethanesulfonic acid) modulates inhibitory neurotransmitter receptors. This study aimed to determine if the dual action of taurine on GABAC-ρ1R relates to its structure. To address this, we tested the ability of the structurally related compounds homotaurine, hypotaurine, and isethionic acid to modulate GABAC-ρ1R. In Xenopus laevis oocytes, hypotaurine and homotaurine partially activate heterologously expressed GABAC-ρ1R, showing an increment in its deactivation time with no changes in channel permeability, whereas isethionic acid showed no effect. Competitive assays suggest that hypotaurine and homotaurine compete for the GABA-binding site. In addition, their effects were blocked by the ion-channel blockers picrotixin and Methyl(1,2,5,6-tetrahydropyridine-4-yl) phosphinic acid. In contrast to taurine, co-application of GABA with hypotaurine or homotaurine revealed that the dual effect is present separately for each compound: hypotaurine modulates positively the GABA current, while homotaurine shows a negative modulation, both in a dose-dependent manner. Interestingly, homotaurine diminished hypotaurine-induced currents. Thus, these results strongly suggest a competitive interaction between GABA and homotaurine or hypotaurine for the same binding site. "In silico" modeling confirms these observations, but it also shows a second binding site for homotaurine, which could explain the negative effect of this compound on the current generated by GABA or hypotaurine, during co-application protocols. The sulfur-containing compounds structurally related to taurine are partial agonists of GABAC-ρ1R that occupy the agonist binding site. The dual effect is unique to taurine, whereas in the case of hypotaurine and homotaurine it presents separately; hypotaurine increases and homotaurine decreases the GABA current.

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The data shown below were collected from the profiles of 3 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 17 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 17 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 6 35%
Student > Bachelor 2 12%
Other 1 6%
Student > Master 1 6%
Professor 1 6%
Other 0 0%
Unknown 6 35%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 2 12%
Agricultural and Biological Sciences 2 12%
Medicine and Dentistry 1 6%
Neuroscience 1 6%
Chemistry 1 6%
Other 0 0%
Unknown 10 59%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 14 June 2023.
All research outputs
#15,166,652
of 25,758,695 outputs
Outputs from BMC Neuroscience
#564
of 1,304 outputs
Outputs of similar age
#176,537
of 342,674 outputs
Outputs of similar age from BMC Neuroscience
#6
of 22 outputs
Altmetric has tracked 25,758,695 research outputs across all sources so far. This one is in the 40th percentile – i.e., 40% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,304 research outputs from this source. They receive a mean Attention Score of 4.7. This one has gotten more attention than average, scoring higher than 55% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 342,674 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 47th percentile – i.e., 47% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 22 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 72% of its contemporaries.