Computer-aided design of selective ligands of the benzodiazepine-binding site of the GABAA receptor (original) (raw)

A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model

Michael Poe

International Journal of Medicinal Chemistry, 2015

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Identification of amino acid residues responsible for the α5 subunit binding selectivity of L‐655,708, a benzodiazepine binding site ligand at the GABAA receptor

Karine Martin

Journal of …, 2001

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Structural Analysis and Binding Modes of Benzodiazepines with Modeled GABAA Receptor Subunit Gamma-2

Rajasekhara Reddy

2014

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Actions of two GABAA receptor benzodiazepine-site ligands that are mediated via non-γ2-dependent modulation

Holger Rabe, Hartmut Lüddens

European Journal of Pharmacology, 2011

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Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes

Uwe Rudolph

Nature Reviews Drug Discovery, 2011

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The use of a pharmacophore model for identification of novel ligands for the benzodiazepine binding site of the GABAA receptor

Michael Howard

Journal of Molecular Graphics and Modelling, 2004

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Are GABAA Receptors Containing α5 Subunits Contributing to the Sedative Properties of Benzodiazepine Site Agonists?

Dubravko Bokonjic

Neuropsychopharmacology, 2008

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Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: The approximated activation of receptor subtypes may explain behavioral effects

Bojan Markovic

Brain Research, 2014

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Determinants of recognition of ligands binding to benzodiazepine receptor/GABAA receptors initiating sedation

James Cook

European Journal of Pharmacology, 2000

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Structural Elements of the gamma -Aminobutyric Acid Type A Receptor Conferring Subtype Selectivity for Benzodiazepine Site Ligands

Pascal George

Journal of Biological Chemistry, 1999

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Structural Elements of the γ-Aminobutyric Acid Type A Receptor Conferring Subtype Selectivity for Benzodiazepine Site Ligands

François BESNARD

Journal of Biological Chemistry, 1999

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Tricyclic pyridones as functionally selective human GABAAα2/3 receptor-ion channel ligands

Andrew Owens

Bioorganic & Medicinal Chemistry Letters, 2004

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Biological function of GABAA/benzodiazepine receptor heterogeneity

Hartmut Lüddens

Journal of Psychiatric Research, 1995

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The γ3-subunit of the GABAA-receptor confers sensitivity to benzodiazepine receptor ligands

Frederic Knoflach

FEBS Letters, 1991

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Conformational changes at benzodiazepine binding sites of GABAA receptors detected with a novel technique

Anne Gonthier

Journal of Neurochemistry, 2005

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Benzodiazepine Binding Site Occupancy by the Novel GABAA Receptor Subtype-Selective Drug 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in Rats, Primates, and Humans

Bindi Sohal

Journal of Pharmacology and Experimental Therapeutics, 2009

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An Updated Unified Pharmacophore Model of the Benzodiazepine Binding Site on γ-Aminobutyric Acida Receptors: Correlation with Comparative Models

James Cook

Current Medicinal Chemistry, 2007

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Benzodiazepine Binding Site Occupancy by the Novel GABAA Receptor Subtype-Selective Drug 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in Rats, Primates, and Humans

Sandra Sanabria Bohórquez

Journal of Pharmacology and Experimental Therapeutics, 2009

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Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABAA α5 inverse agonist series

Frederic Knoflach

Bioorganic & Medicinal Chemistry Letters, 2009

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benzodiazepine receptor ligands a patent review (2006-2012).pdf

Gabriella Guerrini

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A study of the structure–activity relationship of GABAA–benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis

James Cook

Bioorganic & Medicinal Chemistry, 2008

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Selective Influence on Contextual Memory: Physiochemical Properties Associated with Selectivity of Benzodiazepine Ligands at GABA A Receptors Containing the α5 Subunit

James Cook

Journal of Medicinal Chemistry, 2008

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Interaction of SQ 20009 and GABA-like drugs as modulators of benzodiazepine receptor binding

Porntip Supavilai

European Journal of Pharmacology, 1980

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Kucken AM, Wagner DA, Ward PR, Teissere JA, Boileau AJ, Czajkowski C (2000) "Identification of benzodiazepine binding site residues in the gamma2 subunit of the GABA(A) receptor" Molecular Pharmacology 57:932-9.

Jeremy Alden Teissere

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Benzodiazepine receptor ligands: a patent review (2006 – 2012)

Gabriella Guerrini

Expert Opinion on Therapeutic Patents, 2013

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The GABAA receptor and benzodiazepine acceptor site

Michel Bourin

SOJ Pharmacy & Pharmaceutical Sciences, 2018

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Heterogeneity in the Allosteric Interaction Between the ?-Aminobutyric Acid (GABA) Binding Site and Three Different Benzodiazepine Binding Sites of the GABA A /Benzodiazepine Receptor Complex in the Rat Nervous System

Javier Vitorica

Journal of Neurochemistry, 1992

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Affinity of various benzodiazepine site ligands in mice with a point mutation in the GABAA receptor γ2 subunit

Alessandra Oberto

Biochemical Pharmacology, 2004

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