Literature DB >> 21428818

Use of multicomponent reactions in developing small-molecule tools to study GABAA receptor mechanism and function.

Ryan W Lewis1, George P Hess, Bruce Ganem.   

Abstract

We discuss the potential use of multicomponent reactions in developing small-molecule probes of GABA(A) receptor function. Two examples that illustrate this approach are presented: the synthesis of a class of compounds that specifically modulate the function of GABA(A) receptors containing the δ-subunit, and also 'caged' GABA derivatives. A caged GABA is a photolabile precursor of GABA that releases GABA upon photolysis.

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Year:  2011        PMID: 21428818      PMCID: PMC3152297          DOI: 10.4155/fmc.10.302

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   3.808


  60 in total

1.  Dihydropyrimidinone positive modulation of delta-subunit-containing gamma-aminobutyric acid type A receptors, including an epilepsy-linked mutant variant.

Authors:  Ryan W Lewis; John Mabry; Jason G Polisar; Kyle P Eagen; Bruce Ganem; George P Hess
Journal:  Biochemistry       Date:  2010-06-15       Impact factor: 3.162

2.  The beta subunit determines the ion selectivity of the GABAA receptor.

Authors:  Marianne L Jensen; Daniel B Timmermann; Tina H Johansen; Arne Schousboe; Thomas Varming; Philip K Ahring
Journal:  J Biol Chem       Date:  2002-08-12       Impact factor: 5.157

3.  Specific subtypes of GABAA receptors mediate phasic and tonic forms of inhibition in hippocampal pyramidal neurons.

Authors:  George A Prenosil; Edith M Schneider Gasser; Uwe Rudolph; Ruth Keist; Jean-Marc Fritschy; Kaspar E Vogt
Journal:  J Neurophysiol       Date:  2006-08       Impact factor: 2.714

4.  Picrotoxin inhibition mechanism of a gamma-aminobutyric acid A receptor investigated by a laser-pulse photolysis technique.

Authors:  Latha Ramakrishnan; George P Hess
Journal:  Biochemistry       Date:  2005-06-14       Impact factor: 3.162

5.  Synthesis, photophysical, photochemical and biological properties of caged GABA, 4-[[(2H-1-benzopyran-2-one-7-amino-4-methoxy) carbonyl] amino] butanoic acid.

Authors:  Beate Cürten; Paul H M Kullmann; Mark E Bier; Karl Kandler; Brigitte F Schmidt
Journal:  Photochem Photobiol       Date:  2005 May-Jun       Impact factor: 3.421

6.  Discovery of small molecule human C5a receptor antagonists.

Authors:  Hitesh J Sanganee; Andrew Baxter; Simon Barber; Alastair J H Brown; Denise Grice; Fraser Hunt; Sarah King; David Laughton; Garry Pairaudeau; Bob Thong; Richard Weaver; John Unitt
Journal:  Bioorg Med Chem Lett       Date:  2008-12-31       Impact factor: 2.823

7.  Novel compounds selectively enhance delta subunit containing GABA A receptors and increase tonic currents in thalamus.

Authors:  K A Wafford; M B van Niel; Q P Ma; E Horridge; M B Herd; D R Peden; D Belelli; J J Lambert
Journal:  Neuropharmacology       Date:  2008-08-13       Impact factor: 5.250

8.  Novel syntheses of tetrahydrobenzodiazepines and dihydropyrazines via isocyanide-based multicomponent reactions of diamines.

Authors:  Ahmad Shaabani; Ali Maleki; Fatemeh Hajishaabanha; Hamid Mofakham; Mozhdeh Seyyedhamzeh; Mojtaba Mahyari; Seik Weng Ng
Journal:  J Comb Chem       Date:  2010 Jan-Feb

9.  Genuine antihyperalgesia by systemic diazepam revealed by experiments in GABAA receptor point-mutated mice.

Authors:  Julia Knabl; Ulrike B Zeilhofer; Florence Crestani; Uwe Rudolph; Hanns Ulrich Zeilhofer
Journal:  Pain       Date:  2008-12-16       Impact factor: 6.961

10.  Laser photolysis of DPNI-GABA, a tool for investigating the properties and distribution of GABA receptors and for silencing neurons in situ.

Authors:  Federico F Trigo; George Papageorgiou; John E T Corrie; David Ogden
Journal:  J Neurosci Methods       Date:  2009-05-05       Impact factor: 2.390

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