Literature DB >> 17604168

Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.

Jin-Sung Kim1, Anshul Padnya, Maegan Weltzin, Brian W Edmonds, Marvin K Schulte, Richard A Glennon.   

Abstract

Desformylflustrabromine (dFBr; 1) and desformylflustrabromine-B (dFBr-B; 2) have been previously isolated from natural sources, and the former has been demonstrated to be a novel and selective positive allosteric modulator of alpha4beta2 nicotinic acetylcholine (nACh) receptors. The present study describes the synthesis of water-soluble salts of 1 and 2, and confirms and further investigates the actions of 1 and 2 using two-electrode voltage clamp recordings.

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Year:  2007        PMID： 17604168      PMCID： PMC3633077          DOI： 10.1016/j.bmcl.2007.06.047

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  16 in total

1.  Four new bromotryptamine derivatives from the marine bryozoan Flustra foliacea.

Authors:  Lars Peters; Gabriele M König; Heinrich Terlau; Anthony D Wright
Journal:  J Nat Prod       Date:  2002-11       Impact factor: 4.050

Review 2.  2. Medicinal chemistry of alpha4beta2 nicotinic cholinergic receptor ligands.

Authors:  Richard A Glennon
Journal:  Prog Med Chem       Date:  2004

3.  A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization.

Authors:  Raymond S Hurst; Mihaly Hajós; Mario Raggenbass; Theron M Wall; Nicole R Higdon; Judy A Lawson; Karen L Rutherford-Root; Mitchell B Berkenpas; W E Hoffmann; David W Piotrowski; Vincent E Groppi; Geraldine Allaman; Roch Ogier; Sonia Bertrand; Daniel Bertrand; Stephen P Arneric
Journal:  J Neurosci       Date:  2005-04-27       Impact factor: 6.167

4.  Acetylcholine nicotinic receptors: finding the putative binding site of allosteric modulators using the "blind docking" approach.

Authors:  Bogdan Iorga; Denyse Herlem; Elvina Barré; Catherine Guillou
Journal:  J Mol Model       Date:  2005-12-22       Impact factor: 1.810

Review 5.  Molecular mechanisms and binding site locations for noncompetitive antagonists of nicotinic acetylcholine receptors.

Authors:  Hugo R Arias; Pankaj Bhumireddy; Cecilia Bouzat
Journal:  Int J Biochem Cell Biol       Date:  2006-02-20       Impact factor: 5.085

Review 6.  Noncompetitive inhibition of nicotinic acetylcholine receptors by endogenous molecules.

Authors:  H R Arias
Journal:  J Neurosci Res       Date:  1998-05-15       Impact factor: 4.164

Review 7.  Localization of agonist and competitive antagonist binding sites on nicotinic acetylcholine receptors.

Authors:  H R Arias
Journal:  Neurochem Int       Date:  2000-06       Impact factor: 3.921

Review 8.  Unconventional ligands and modulators of nicotinic receptors.

Authors:  Edna F R Pereira; Corey Hilmas; Mariton D Santos; Manickavasagom Alkondon; Alfred Maelicke; Edson X Albuquerque
Journal:  J Neurobiol       Date:  2002-12

9.  Potentiation of human alpha4beta2 neuronal nicotinic receptors by a Flustra foliacea metabolite.

Authors:  Francisco Sala; José Mulet; Krishna P Reddy; José Antonio Bernal; Philip Wikman; Luis Miguel Valor; Lars Peters; Gabriele M König; Manuel Criado; Salvador Sala
Journal:  Neurosci Lett       Date:  2005-01-10       Impact factor: 3.046

10.  Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.

Authors:  Marek Samochocki; Anja Höffle; Andreas Fehrenbacher; Ruth Jostock; Jürgen Ludwig; Claudia Christner; Martin Radina; Marion Zerlin; Christoph Ullmer; Edna F R Pereira; Hermann Lübbert; Edson X Albuquerque; Alfred Maelicke
Journal:  J Pharmacol Exp Ther       Date:  2003-03-20       Impact factor: 4.030
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  25 in total

1.  Allosteric modulation of alpha4beta2 nicotinic acetylcholine receptors by HEPES.

Authors:  Maegan M Weltzin; Yanzhou Huang; Marvin K Schulte
Journal:  Eur J Pharmacol       Date:  2012-06-23       Impact factor: 4.432

2.  Desformylflustrabromine (dFBr) and [3H]dFBr-Labeled Binding Sites in a Nicotinic Acetylcholine Receptor.

Authors:  Ayman K Hamouda; Ze-Jun Wang; Deirdre S Stewart; Atul D Jain; Richard A Glennon; Jonathan B Cohen
Journal:  Mol Pharmacol       Date:  2015-04-13       Impact factor: 4.436

Review 3.  Orthosteric and allosteric potentiation of heteromeric neuronal nicotinic acetylcholine receptors.

Authors:  Jingyi Wang; Jon Lindstrom
Journal:  Br J Pharmacol       Date:  2017-03-20       Impact factor: 8.739

Review 4.  Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.

Authors:  Dustin K Williams; Jingyi Wang; Roger L Papke
Journal:  Biochem Pharmacol       Date:  2011-05-14       Impact factor: 5.858

5.  Effects of nicotine in combination with drugs described as positive allosteric nicotinic acetylcholine receptor modulators in vitro: discriminative stimulus and hypothermic effects in mice.

Authors:  Megan J Moerke; Fernando B de Moura; Wouter Koek; Lance R McMahon
Journal:  Eur J Pharmacol       Date:  2016-05-27       Impact factor: 4.432

6.  Levamisole: A Positive Allosteric Modulator for the α3β4 Nicotinic Acetylcholine Receptors Prevents Weight Gain in the CD-1 Mice on a High Fat Diet.

Authors:  Jeanne A Lewis; Jerrel L Yakel; Anshul A Pandya
Journal:  Curr Pharm Des       Date:  2017       Impact factor: 3.116

7.  Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT₁a receptor antagonist.

Authors:  Anshul A Pandya; Jerrel L Yakel
Journal:  Neuropharmacology       Date:  2013-01-12       Impact factor: 5.250

Review 8.  Recent progress in neuroactive marine natural products.

Authors:  Ryuichi Sakai; Geoffrey T Swanson
Journal:  Nat Prod Rep       Date:  2014-01-17       Impact factor: 13.423

9.  Positive allosteric modulation of α4β2 nicotinic acetylcholine receptors as a new approach to smoking reduction: evidence from a rat model of nicotine self-administration.

Authors:  Xiu Liu
Journal:  Psychopharmacology (Berl)       Date:  2013-05-28       Impact factor: 4.530

10.  Photolabeling a Nicotinic Acetylcholine Receptor (nAChR) with an (α4)3(β2)2 nAChR-Selective Positive Allosteric Modulator.

Authors:  Ayman K Hamouda; Farah Deba; Ze-Jun Wang; Jonathan B Cohen
Journal:  Mol Pharmacol       Date:  2016-03-14       Impact factor: 4.436
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