Search Results - "Forman, Stuart"
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γ-Aminobutyric Acid Type A Receptor Subtypes and Circuit Connections in Midazolam-induced Amnesia, Sedation, and Hypnosis
Published in Anesthesiology (Philadelphia) (01-06-2022)Get full text
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Clinical and Molecular Pharmacology of Etomidate
Published in Anesthesiology (Philadelphia) (01-03-2011)“…This review focuses on the unique clinical and molecular pharmacologic features of etomidate. Among general anesthesia induction drugs, etomidate is the only…”
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Systematized Serendipity: Fishing Expeditions for Anesthetic Drugs and Targets
Published in Anesthesiology (Philadelphia) (01-11-2024)“…Most of science involves making observations, forming hypotheses, and testing those hypotheses, to form valid conclusions. However, a distinct, longstanding,…”
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Mapping General Anesthetic Sites in Heteromeric γ-Aminobutyric Acid Type A Receptors Reveals a Potential For Targeting Receptor Subtypes
Published in Anesthesia and analgesia (01-11-2016)“…IV general anesthetics, including propofol, etomidate, alphaxalone, and barbiturates, produce important actions by enhancing γ-aminobutyric acid type A (GABAA)…”
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New Evidence of Receptor-based Pharmacology Underlying a Volatile Anesthetic Effect
Published in Anesthesiology (Philadelphia) (01-11-2020)Get full text
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Correction for Inhibition Leads to an Allosteric Co-Agonist Model for Pentobarbital Modulation and Activation of α1β3γ2L GABAA Receptors
Published in PloS one (25-04-2016)“…Pentobarbital, like propofol and etomidate, produces important general anesthetic effects through GABAA receptors. Photolabeling also indicates that…”
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Competitive Interactions Between Propofol and Diazepam: Studies in GABA A Receptors and Zebrafish
Published in The Journal of pharmacology and experimental therapeutics (01-12-2022)“…Although propofol is among the most commonly administered general anesthetics, its mechanism of action is not fully understood. It has been hypothesized that…”
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Selective actions of benzodiazepines at the transmembrane anaesthetic binding sites of the GABA A receptor: In vitro and in vivo studies
Published in British journal of pharmacology (01-12-2021)“…In addition to binding to the classical high-affinity extracellular benzodiazepine binding site of the GABA receptor, some benzodiazepines occupy transmembrane…”
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Etomidate Effects on Desensitization and Deactivation of α 4 β 3 δ GABA A Receptors Inducibly Expressed in HEK293 TetR Cells
Published in The Journal of pharmacology and experimental therapeutics (01-01-2019)“…Central 4 receptors are the most abundant isoform of subunit-containing extrasynaptic GABA receptors that mediate tonic inhibition. Although the amplitude of…”
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Substituted Cysteine Modification and Protection with n -Alkyl- Methanethiosulfonate Reagents Yields a Precise Estimate of the Distance between Etomidate and a Residue in Activated GABA Type A Receptors
Published in Molecular pharmacology (01-06-2021)“…The anesthetic etomidate modulates synaptic 1 2/3 2 GABA receptors via binding sites located in transmembrane +/ - interfaces. Various approaches indicate that…”
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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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γ-Amino Butyric Acid Type A Receptor Mutations at β2N265 Alter Etomidate Efficacy While Preserving Basal and Agonist-dependent Activity
Published in Anesthesiology (Philadelphia) (01-10-2009)“…Background Etomidate acts at gamma-Aminobutyric acid type A (GABAA) receptors containing beta2 or beta3, but not beta1 subunits. Mutations at beta residue 265…”
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Monod-Wyman-Changeux Allosteric Shift Analysis in Mutant α 1 β 3 γ 2L GABA A Receptors Indicates Selectivity and Crosstalk among Intersubunit Transmembrane Anesthetic Sites
Published in Molecular pharmacology (01-04-2019)“…Propofol, etomidate, and barbiturate anesthetics are allosteric coagonists at pentameric 1 3 2 GABA receptors, modulating channel activation via four…”
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Tethering IL2 to Its Receptor IL2Rβ Enhances Antitumor Activity and Expansion of Natural Killer NK92 Cells
Published in Cancer research (Chicago, Ill.) (01-11-2017)“…IL2 is an immunostimulatory cytokine for key immune cells including T cells and natural killer (NK) cells. Systemic IL2 supplementation could enhance…”
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Mechanisms of Actions of Inhaled Anesthetics
Published in The New England journal of medicine (22-05-2003)“…“Suffering so great as I underwent cannot be expressed in words . . . but the blank whirlwind of emotion, the horror of great darkness, and the sense of…”
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Mutations at beta N265 in γ-aminobutyric acid type A receptors alter both binding affinity and efficacy of potent anesthetics
Published in PloS one (27-10-2014)“…Etomidate and propofol are potent general anesthetics that act via GABAA receptor allosteric co-agonist sites located at transmembrane β+/α- inter-subunit…”
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Anesthetic sites and allosteric mechanisms of action on Cys-loop ligand-gated ion channels
Published in Canadian journal of anesthesia (01-02-2011)“…Purpose The Cys-loop ligand-gated ion channel superfamily is a major group of neurotransmitter-activated receptors in the central and peripheral nervous…”
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Anesthetics target interfacial transmembrane sites in nicotinic acetylcholine receptors
Published in Neuropharmacology (01-09-2015)“…General anesthetics are a heterogeneous group of small amphiphilic ligands that interact weakly at multiple allosteric sites on many pentameric ligand gated…”
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Drug-selective Anesthetic Insensitivity of Zebrafish Lacking γ-Aminobutyric Acid Type A Receptor β3 Subunits
Published in Anesthesiology (Philadelphia) (01-12-2019)“…BACKGROUND:Transgenic mouse studies suggest that γ-aminobutyric acid type A (GABAA) receptors containing β3 subunits mediate important effects of etomidate,…”
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Tryptophan and Cysteine Mutations in M1 Helices of α1β3γ2L γ-Aminobutyric Acid Type A Receptors Indicate Distinct Intersubunit Sites for Four Intravenous Anesthetics and One Orphan Site
Published in Anesthesiology (Philadelphia) (01-12-2016)“…BACKGROUND:γ-Aminobutyric acid type A (GABAA) receptors mediate important effects of intravenous general anesthetics. Photolabel derivatives of etomidate,…”
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