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Analysis of Modulation of the ρ1 GABA_A Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites.

ABSTRACT: The ρ1 GABA_A receptor is prominently expressed in the retina and is present at lower levels in several brain regions and other tissues. Although the ρ1 receptor is insensitive to many anesthetic drugs that modulate the heteromeric GABA_A receptor, it maintains a rich and multifaceted steroid pharmacology. The receptor is negatively modulated by 5β-reduced steroids, sulfated or carboxylated steroids, and β-estradiol, whereas many 5α-reduced steroids potentiate the receptor. In this study, we analyzed modulation of the human ρ1 GABA_A receptor by several neurosteroids, individually and in combination, in the framework of the coagonist concerted transition model. Experiments involving coapplication of two or more steroid

SUBMITTER: Germann AL

PROVIDER: S-EPMC7472123 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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Dataset Information

Analysis of Modulation of the ρ1 GABA_A Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

Analysis of Modulation of the ρ1 GABAA Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Analysis of Modulation of the ρ1 GABA_A Receptor by Combinations of Inhibitory and Potentiating Neurosteroids Reveals Shared and Distinct Binding Sites.