Logo image
Long‐term regulation of voltage‐gated Ca2+ channels by gabapentin
Journal article   Open access   Peer reviewed

Long‐term regulation of voltage‐gated Ca2+ channels by gabapentin

Myoung-Goo Kang, Ricardo Felix and Kevin P Campbell
FEBS letters, Vol.528(1-3), pp.177-182
09/25/2002
DOI: 10.1016/S0014-5793(02)03295-7
PMID: 12297300
url
https://doi.org/10.1016/S0014-5793(02)03295-7View
Published (Version of record) Open Access

Abstract

Gabapentin (GBP) is a γ‐aminobutyric acid analog effective in the treatment of seizures. A high‐affinity interaction between GBP and the α2δ subunit of the voltage‐gated Ca2+ channels has been documented. In this report, we examined the effects of the chronic treatment with GBP on neuronal recombinant P/Q‐type Ca2+ channels expressed in Xenopus oocytes. GBP did not affect significantly the amplitude or the voltage dependence of the currents. Exposure to the drug did, however, slow down the kinetics of inactivation in a dose‐dependent fashion. In addition, biochemical analysis showed that the integrity of Ca2+ channel complex is not apparently affected by GBP binding, suggesting that chronic treatment with the drug might cause the channel kinetic modification through subtle conformational changes of the protein complex.
ω-Conotoxin CaV2.1 subunit Gabapentin Epilepsy Ca2+ channel α2δ subunit

Details

Metrics

Logo image