Search Results - "Germann, Allison L."
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Multiple functional neurosteroid binding sites on GABAA receptors
Published in PLoS biology (01-03-2019)“…Neurosteroids are endogenous modulators of neuronal excitability and nervous system development and are being developed as anesthetic agents and treatments for…”
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Modulation of the mammalian GABAA receptor by type I and type II positive allosteric modulators of the α7 nicotinic acetylcholine receptor
Published in British journal of pharmacology (01-12-2022)“…Background and Purpose Positive allosteric modulators of the α7 nicotinic acetylcholine (nACh) receptor (α7‐PAMs) possess promnesic and procognitive properties…”
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Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABAA Receptor: Relating Occupancy to State Functions
Published in Molecular pharmacology (01-10-2020)“…Muscimol is a psychoactive isoxazole derived from the mushroom Amanita muscaria and a potent orthosteric agonist of the GABAA receptor. The binding of…”
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4
Site-specific effects of neurosteroids on GABAA receptor activation and desensitization
Published in eLife (21-09-2020)“…This study examines how site-specific binding to three identified neurosteroid-binding sites in the α 1 β 3 GABA A receptor (GABA A R) contributes to…”
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Application of the Co-Agonist Concerted Transition Model to Analysis of GABAA Receptor Properties
Published in Current neuropharmacology (2019)“…The co-agonist concerted transition model is a simple and practical solution to analyze various aspects of GABAA receptor function. Several model-based…”
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Multiple Non-Equivalent Interfaces Mediate Direct Activation of GABAA Receptors by Propofol
Published in Current neuropharmacology (01-10-2016)“…Background: Propofol is a sedative agent that at clinical concentrations acts by allosterically activating or potentiating the ?-aminobutyric acid type A…”
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Activation of the α1β2γ2L GABAA Receptor by Physiological Agonists
Published in Biomolecules (Basel, Switzerland) (11-12-2021)“…The Cl− permeable GABAA receptor is a major contributor to cellular inhibition in the brain. The receptor is normally activated by synaptically-released or…”
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Activation of the Rat α1β2ε GABAA Receptor by Orthosteric and Allosteric Agonists
Published in Biomolecules (Basel, Switzerland) (21-06-2022)“…GABAA receptors are a major contributor to fast inhibitory neurotransmission in the brain. The receptors are activated upon binding the transmitter GABA or…”
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Mutational Analysis of Anesthetic Binding Sites and Their Effects on GABAA Receptor Activation and Modulation by Positive Allosteric Modulators of the α7 Nicotinic Receptor
Published in Biomolecules (Basel, Switzerland) (20-04-2023)“…The positive allosteric modulators (PAMs) of the α7 nicotinic receptor N-(5-Cl-2-hydroxyphenyl)-N′-[2-Cl-5-(trifluoromethyl)phenyl]-urea (NS-1738) and…”
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The Mechanism of Enantioselective Neurosteroid Actions on GABAA Receptors
Published in Biomolecules (Basel, Switzerland) (09-02-2023)“…The neurosteroid allopregnanolone (ALLO) and pregnanolone (PREG), are equally effective positive allosteric modulators (PAMs) of GABAA receptors…”
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Steady‐state activation and modulation of the synaptic‐type α1β2γ2L GABAA receptor by combinations of physiological and clinical ligands
Published in Physiological reports (01-09-2019)“…The synaptic α1β2γ2 GABAA receptor is activated phasically by presynaptically released GABA. The receptor is considered to be inactive between synaptic events…”
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Potentiation of the GABA A R reveals variable energetic contributions by etiocholanolone and propofol
Published in Biophysical journal (16-07-2024)“…The properties of a potentiator are typically evaluated by measuring its ability to enhance the magnitude of the control response. Analysis of the ability of…”
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13
The Actions of Drug Combinations on the GABA A Receptor Manifest as Curvilinear Isoboles of Additivity
Published in Molecular pharmacology (01-11-2017)“…Drug interactions are often analyzed in terms of isobolograms. In the isobologram, the line connecting the axial points corresponding to the concentrations of…”
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The Sulfated Steroids Pregnenolone Sulfate and Dehydroepiandrosterone Sulfate Inhibit the α 1 β 3 γ 2L GABA A Receptor by Stabilizing a Novel Nonconducting State
Published in Molecular pharmacology (01-02-2022)“…The GABA receptor is inhibited by the endogenous sulfated steroids pregnenolone sulfate (PS) and dehydroepiandrosterone sulfate (DHEAS). It has been proposed…”
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The Sulfated Steroids Pregnenolone Sulfate and Dehydroepiandrosterone Sulfate Inhibit the α1β3γ2L GABAA Receptor by Stabilizing a Novel Nonconducting State
Published in Molecular pharmacology (01-02-2022)“…The GABA A receptor is inhibited by the endogenous sulfated steroids pregnenolone sulfate (PS) and dehydroepiandrosterone sulfate (DHEAS). It has been proposed…”
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Analysis of GABA A Receptor Activation by Combinations of Agonists Acting at the Same or Distinct Binding Sites
Published in Molecular pharmacology (01-01-2019)“…Under both physiologic and clinical conditions GABA receptors are exposed to multiple agonists, including the transmitter GABA, endogenous or exogenous…”
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Chemical, Pharmacological, and Structural Characterization of Novel Acrylamide-Derived Modulators of the GABAA Receptor
Published in Molecular pharmacology (01-09-2023)“…Acrylamide-derived compounds have been previously shown to act as modulators of members of the Cys-loop transmitter-gated ion channel family, including the…”
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Propofol Is an Allosteric Agonist with Multiple Binding Sites on Concatemeric Ternary GABA A Receptors
Published in Molecular pharmacology (01-02-2018)“…GABA receptors can be directly activated and potentiated by the intravenous anesthetic propofol. Previous photolabeling, modeling, and functional data have…”
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Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABA A Receptor: Relating Occupancy to State Functions
Published in Molecular pharmacology (01-10-2020)“…Muscimol is a psychoactive isoxazole derived from the mushroom and a potent orthosteric agonist of the GABA receptor. The binding of [ H]muscimol has been used…”
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20
Steady-state activation of the high-affinity isoform of the α4β2δ GABAA receptor
Published in Scientific reports (05-11-2019)“…Activation of GABA A receptors consisting of α4, β2 (or β3), and δ subunits is a major contributor to tonic inhibition in several brain regions. The goal of…”
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