Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists

The Cl<sup<−</sup< permeable GABA<sub<A</sub< receptor is a major contributor to cellular inhibition in the brain. The receptor is normally activated by synaptically-released or ambient GABA but is sensitive to a number of physiological compounds such as β-alanine, taurine, a...
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Autor*in:	Spencer R. Pierce [verfasserIn] Allison L. Germann [verfasserIn] Gustav Akk [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2021

Schlagwörter:	GABA activation potentiation orthosteric agonist allosteric agonist

Übergeordnetes Werk:	In: Biomolecules - MDPI AG, 2013, 11(2021), 12, p 1864
Übergeordnetes Werk:	volume:11 ; year:2021 ; number:12, p 1864

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/biom11121864

Katalog-ID:	DOAJ069363366

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language	English
source	In Biomolecules 11(2021), 12, p 1864 volume:11 year:2021 number:12, p 1864
sourceStr	In Biomolecules 11(2021), 12, p 1864 volume:11 year:2021 number:12, p 1864
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	GABA<sub<A</sub< receptor activation potentiation orthosteric agonist allosteric agonist Microbiology
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container_title	Biomolecules
authorswithroles_txt_mv	Spencer R. Pierce @@aut@@ Allison L. Germann @@aut@@ Gustav Akk @@aut@@
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author	Spencer R. Pierce
spellingShingle	Spencer R. Pierce misc QR1-502 misc GABA<sub<A</sub< receptor misc activation misc potentiation misc orthosteric agonist misc allosteric agonist misc Microbiology Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists
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topic_title	QR1-502 Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists GABA<sub<A</sub< receptor activation potentiation orthosteric agonist allosteric agonist
topic	misc QR1-502 misc GABA<sub<A</sub< receptor misc activation misc potentiation misc orthosteric agonist misc allosteric agonist misc Microbiology
topic_unstemmed	misc QR1-502 misc GABA<sub<A</sub< receptor misc activation misc potentiation misc orthosteric agonist misc allosteric agonist misc Microbiology
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title	Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists
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title_auth	Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists
abstract	The Cl<sup<−</sup< permeable GABA<sub<A</sub< receptor is a major contributor to cellular inhibition in the brain. The receptor is normally activated by synaptically-released or ambient GABA but is sensitive to a number of physiological compounds such as β-alanine, taurine, and neurosteroids that, to various degrees, activate the receptor and modulate responses either to the transmitter or to each other. Here, we describe α1β2γ2L GABA<sub<A</sub< receptor activation and modulation by combinations of orthosteric and allosteric activators. The overall goal was to gain insight into how changes in the levels of endogenous agonists modulate receptor activity and influence cellular inhibition. Experimental observations and simulations are described in the framework of a cyclic concerted transition model. We also provide general analytical solutions for the analysis of electrophysiological data collected in the presence of combinations of active compounds.
abstractGer	The Cl<sup<−</sup< permeable GABA<sub<A</sub< receptor is a major contributor to cellular inhibition in the brain. The receptor is normally activated by synaptically-released or ambient GABA but is sensitive to a number of physiological compounds such as β-alanine, taurine, and neurosteroids that, to various degrees, activate the receptor and modulate responses either to the transmitter or to each other. Here, we describe α1β2γ2L GABA<sub<A</sub< receptor activation and modulation by combinations of orthosteric and allosteric activators. The overall goal was to gain insight into how changes in the levels of endogenous agonists modulate receptor activity and influence cellular inhibition. Experimental observations and simulations are described in the framework of a cyclic concerted transition model. We also provide general analytical solutions for the analysis of electrophysiological data collected in the presence of combinations of active compounds.
abstract_unstemmed	The Cl<sup<−</sup< permeable GABA<sub<A</sub< receptor is a major contributor to cellular inhibition in the brain. The receptor is normally activated by synaptically-released or ambient GABA but is sensitive to a number of physiological compounds such as β-alanine, taurine, and neurosteroids that, to various degrees, activate the receptor and modulate responses either to the transmitter or to each other. Here, we describe α1β2γ2L GABA<sub<A</sub< receptor activation and modulation by combinations of orthosteric and allosteric activators. The overall goal was to gain insight into how changes in the levels of endogenous agonists modulate receptor activity and influence cellular inhibition. Experimental observations and simulations are described in the framework of a cyclic concerted transition model. We also provide general analytical solutions for the analysis of electrophysiological data collected in the presence of combinations of active compounds.
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title_short	Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists
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Activation of the α1β2γ2L GABA<sub<A</sub< Receptor by Physiological Agonists

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