Literature DB >> 20607120

Novel modulator of Na(V)1.1 and Na(V)1.2 Na channels in rat neuronal cells.

Hua Mao1, Lynne A Fieber, Robert E Gawley.   

Abstract

A novel modulator of sodium ion currents was synthesized in 6 steps from a protected dihydroxypyrrolidine nitrone, via 1,3-dipolar cycloaddition reaction with acrylamide. Sodium ion currents in B50 cells were evaluated in comparison to saxitoxin and tetrodotoxin, and revealed an IC(50) of 15.7 muM. The new compound shows no evidence of binding to the C-lobe of the saxitoxin-binding protein saxiphilin.

Entities:  

Year:  2010        PMID： 20607120      PMCID： PMC2894714          DOI： 10.1021/ml100035t

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  13 in total

Review 1.  From ionic currents to molecular mechanisms: the structure and function of voltage-gated sodium channels.

Authors:  W A Catterall
Journal:  Neuron       Date:  2000-04       Impact factor: 17.173

2.  Mutual binding inhibition of tetrodotoxin and saxitoxin to their binding protein from the plasma of the puffer fish, Fugu pardalis.

Authors:  Mari Yotsu-Yamashita; Yuki Shoji; Takahiro Terakawa; Shunichi Yamada; Teruo Miyazawa; Takeshi Yasumoto
Journal:  Biosci Biotechnol Biochem       Date:  2002-11       Impact factor: 2.043

3.  Visible fluorescence chemosensor for saxitoxin.

Authors:  Robert E Gawley; Hua Mao; M Mahbubul Haque; John B Thorne; Jennifer S Pharr
Journal:  J Org Chem       Date:  2007-02-14       Impact factor: 4.354

Review 4.  Future potential and status of selective sodium channel blockers for the treatment of pain.

Authors:  Birgit T Priest
Journal:  Curr Opin Drug Discov Devel       Date:  2009-09

5.  Clonal cell lines from the rat central nervous system.

Authors:  D Schubert; S Heinemann; W Carlisle; H Tarikas; B Kimes; J Patrick; J H Steinbach; W Culp; B L Brandt
Journal:  Nature       Date:  1974-05-17       Impact factor: 49.962

Review 6.  Voltage-gated sodium channel blockers for the treatment of neuropathic pain.

Authors:  Theodore R Cummins; Anthony M Rush
Journal:  Expert Rev Neurother       Date:  2007-11       Impact factor: 4.618

7.  Expression of saxiphilin in insect cells and localization of the saxitoxin-binding site to the C-terminal domain homologous to the C-lobe of transferrins.

Authors:  M A Morabito; L E Llewellyn; E G Moczydlowski
Journal:  Biochemistry       Date:  1995-10-10       Impact factor: 3.162

8.  Dynamics of saxitoxin binding to saxiphilin c-lobe reveals conformational change.

Authors:  Penny Lewis; Ingrid Fritsch; Robert E Gawley; Ralph Henry; Alicia Kight; Jackson O Lay; Rohana Liyanage; Jeanne McLachlin
Journal:  Toxicon       Date:  2007-10-09       Impact factor: 3.033

9.  A structural model of the tetrodotoxin and saxitoxin binding site of the Na+ channel.

Authors:  G M Lipkind; H A Fozzard
Journal:  Biophys J       Date:  1994-01       Impact factor: 4.033

10.  Signal amplification in a microchannel from redox cycling with varied electroactive configurations of an individually addressable microband electrode array.

Authors:  Penny M Lewis; Leah Bullard Sheridan; Robert E Gawley; Ingrid Fritsch
Journal:  Anal Chem       Date:  2010-03-01       Impact factor: 6.986
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  2 in total

1.  A stereocontrolled synthesis of (+)-saxitoxin.

Authors:  Vasudev R Bhonde; Ryan E Looper
Journal:  J Am Chem Soc       Date:  2011-11-23       Impact factor: 15.419

2.  An efficient total synthesis of a potent anti-inflammatory agent, benzocamphorin F, and its anti-inflammatory activity.

Authors:  Yu-Ren Liao; Ping-Chung Kuo; Jun-Weil Liang; Yuh-Chiang Shen; Tian-Shung Wu
Journal:  Int J Mol Sci       Date:  2012-08-21       Impact factor: 6.208
  2 in total

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