Literature DB >> 12363200

Down-regulation of N-type voltage-activated Ca2+ channels by gabapentin.

Alfonso Vega-Hernández1, Ricardo Felix.   

Abstract

1. Although the cellular and molecular mechanisms of the anticonvulsant action of gabapentin (GBP) remain incompletely described, in vitro studies have shown that GBP binds to the alpha2delta subunit of the high voltage-activated (HVA) Ca2+ channels. 2. In this report, we analyzed the effects of GBP on the functional expression of HVA Ca2+ channels in the PC12 cell line model system. Negligible inhibition of Ca2+ channel activity was observed after acute treatment, but a significant decrease in Ca2+ current amplitude was promoted by chronic exposure to GBP. 3. Consistent with this, radioligand binding experiments showed a comparable reduction in the total number of membrane HVA N-type channels after GBP treatment.

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Year:  2002        PMID： 12363200     DOI： 10.1023/a:1019865822069

Source DB:  PubMed          Journal:  Cell Mol Neurobiol        ISSN： 0272-4340            Impact factor:   5.046


  16 in total

Review 1.  A summary of mechanistic hypotheses of gabapentin pharmacology.

Authors:  C P Taylor; N S Gee; T Z Su; J D Kocsis; D F Welty; J P Brown; D J Dooley; P Boden; L Singh
Journal:  Epilepsy Res       Date:  1998-02       Impact factor: 3.045

2.  Dual function of the voltage-dependent Ca2+ channel alpha 2 delta subunit in current stimulation and subunit interaction.

Authors:  C A Gurnett; M De Waard; K P Campbell
Journal:  Neuron       Date:  1996-02       Impact factor: 17.173

3.  The effects of gabapentin on different ligand- and voltage-gated currents in isolated cortical neurons.

Authors:  A Stefani; F Spadoni; P Giacomini; F Lavaroni; G Bernardi
Journal:  Epilepsy Res       Date:  2001-03       Impact factor: 3.045

4.  Differential effect of gabapentin on neuronal and muscle calcium currents.

Authors:  K J Alden; J García
Journal:  J Pharmacol Exp Ther       Date:  2001-05       Impact factor: 4.030

5.  Expression and subunit interaction of voltage-dependent Ca2+ channels in PC12 cells.

Authors:  H Liu; R Felix; C A Gurnett; M De Waard; D R Witcher; K P Campbell
Journal:  J Neurosci       Date:  1996-12-01       Impact factor: 6.167

Review 6.  Gabapentin.

Authors:  M J McLean
Journal:  Epilepsia       Date:  1995       Impact factor: 5.864

7.  Gabapentin inhibits high-threshold calcium channel currents in cultured rat dorsal root ganglion neurones.

Authors:  K G Sutton; D J Martin; R D Pinnock; K Lee; R H Scott
Journal:  Br J Pharmacol       Date:  2002-01       Impact factor: 8.739

8.  Differential expression by nerve growth factor of two types of Ca2+ channels in rat phaeochromocytoma cell lines.

Authors:  M M Usowicz; H Porzig; C Becker; H Reuter
Journal:  J Physiol       Date:  1990-07       Impact factor: 5.182

9.  Electrophysiological and pharmacological properties of the human brain type IIA Na+ channel expressed in a stable mammalian cell line.

Authors:  X Xie; T J Dale; V H John; H L Cater; T C Peakman; J J Clare
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10.  The novel anticonvulsant drug, gabapentin (Neurontin), binds to the alpha2delta subunit of a calcium channel.

Authors:  N S Gee; J P Brown; V U Dissanayake; J Offord; R Thurlow; G N Woodruff
Journal:  J Biol Chem       Date:  1996-03-08       Impact factor: 5.157
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  15 in total

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Authors:  Ian W Rodger
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Journal:  Cell Calcium       Date:  2011-11-03       Impact factor: 6.817

3.  Gabapentin inhibits catecholamine release from adrenal chromaffin cells.

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Journal:  Anesthesiology       Date:  2012-05       Impact factor: 7.892

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Journal:  Anesth Analg       Date:  2011-03-08       Impact factor: 5.108

5.  Gabapentin decreases epileptiform discharges in a chronic model of neocortical trauma.

Authors:  Huifang Li; Kevin D Graber; Sha Jin; Whitney McDonald; Ben A Barres; David A Prince
Journal:  Neurobiol Dis       Date:  2012-07-02       Impact factor: 5.996

6.  Isolation and characterization of the 5´-upstream region of the human voltage-gated Ca(2+) channel α 2δ-1 auxiliary subunit gene: promoter analysis and regulation by transcription factor Sp1.

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7.  Pharmacological disruption of calcium channel trafficking by the alpha2delta ligand gabapentin.

Authors:  Jan Hendrich; Alexandra Tran Van Minh; Fay Heblich; Manuela Nieto-Rostro; Katrin Watschinger; Jörg Striessnig; Jack Wratten; Anthony Davies; Annette C Dolphin
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8.  Regulation of high-voltage-activated Ca2+ channel function, trafficking, and membrane stability by auxiliary subunits.

Authors:  Ricardo Felix; Aida Calderón-Rivera; Arturo Andrade
Journal:  Wiley Interdiscip Rev Membr Transp Signal       Date:  2013-09-01

9.  The alpha(2)delta subunit augments functional expression and modifies the pharmacology of Ca(V)1.3 L-type channels.

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Journal:  Cell Calcium       Date:  2009-09-30       Impact factor: 6.817

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Authors:  Anthony Davies; Leon Douglas; Jan Hendrich; Jack Wratten; Alexandra Tran Van Minh; Isabelle Foucault; Dietlind Koch; Wendy S Pratt; Helen R Saibil; Annette C Dolphin
Journal:  J Neurosci       Date:  2006-08-23       Impact factor: 6.167
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