ArticleMolecular pharmacology2010
Site-specific fluorescence reveals distinct structural changes induced in the human rho 1 GABA receptor by inhibitory neurosteroids.
Article in Molecular pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 14 citations in OpenAlex.
- Voltage-clamp fluorometry for advancing mechanistic understanding of ion channel mechanisms with a focus on acid-sensing ion channels.Biochemical Society transactions · 2024Review
- Inhibitory Actions of Potentiating Neuroactive Steroids in the Human α1β3γ2L γ-Aminobutyric Acid Type A Receptor.Molecular pharmacology · 2024Article
- UNC-49 is a redox-sensitive GABAScience advances · 2023Article
- A new molecular risk pathway for postpartum mood disorders: clues from steroid sulfatase-deficient individuals.Archives of women's mental health · 2021Review
- Conformational dynamics and role of the acidic pocket in ASIC pH-dependent gating.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Identification of an Inhibitory Alcohol Binding Site in GABAA ρ1 Receptors.ACS chemical neuroscience · 2016Article
- Modulation of the human ρ1 GABAA receptor by inhibitory steroids.Psychopharmacology · 2014Article
- Structural studies of the actions of anesthetic drugs on the γ-aminobutyric acid type A receptor.Anesthesiology · 2011Review
- Pharmacology of structural changes at the GABA(A) receptor transmitter binding site.British journal of pharmacology · 2011Article
- Neurosteroids and GABA-A Receptor Function.Frontiers in endocrinology · 2011Article
- Mechanism of Allosteric Modulation of the Cys-loop Receptors.Pharmaceuticals (Basel, Switzerland) · 2010Review
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
The rho 1 GABA receptor is inhibited by a number of neuroactive steroids. A previous study (J Pharmacol Exp Ther 323:236-247, 2007) focusing on the electrophysiological effects of inhibitory steroids on the rho 1 receptor found that steroid inhibitors could be divided into three major groups based on how mutations to residues in the M2 transmembrane domain modified inhibition. It was proposed that the steroids act through distinct mechanisms. We selected representatives of the three groups (pregnanolone, tetrahydrodeoxycorticosterone, pregnanolone sulfate, allopregnanolone sulfate, and beta-estradiol) and probed how these steroids, as well as the nonsteroidal inhibitor picrotoxinin, modify GABA-elicited fluorescence changes from the Alexa 546 C5 maleimide fluorophore attached to residues in the extracellular region of the receptor. The fluorophore responds with changes in quantum yield to changes in the environment, allowing it to probe for structural changes taking place during channel activation or modulation. The results indicate that the modulators have specific effects on fluorescence changes suggesting that distinct conformational changes accompany inhibition. The findings are consistent with the steroids acting as allosteric inhibitors of the rho 1 GABA receptor and support the hypothesis that divergent mechanisms underlie the action of inhibitory steroids on the rho 1 GABA receptor.
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