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. 2002 Apr;22(2):185–190. doi: 10.1023/A:1019865822069

Down-Regulation of N-Type Voltage-Activated Ca2+ Channels by Gabapentin

Alfonso Vega-Hernández 1, Ricardo Felix 1
PMCID: PMC11533754  PMID: 12363200

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 α2 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.

Keywords: Ca2+ channels, gabapentin, ω-conotoxin GVIA, PC12 cells

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