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

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.

journal_name

Cell Mol Neurobiol

authors

Vega-Hernández A,Felix R

doi

10.1023/a:1019865822069

subject

Has Abstract

pub_date

2002-04-01 00:00:00

pages

185-90

issue

2

eissn

0272-4340

issn

1573-6830

journal_volume

22

pub_type

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