Long-term regulation of voltage-gated Ca(2+) channels by gabapentin.

Abstract:

:Gabapentin (GBP) is a gamma-aminobutyric acid analog effective in the treatment of seizures. A high-affinity interaction between GBP and the alpha(2)delta subunit of the voltage-gated Ca(2+) channels has been documented. In this report, we examined the effects of the chronic treatment with GBP on neuronal recombinant P/Q-type Ca(2+) 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 Ca(2+) 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.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Kang MG,Felix R,Campbell KP

doi

10.1016/s0014-5793(02)03295-7

keywords:

subject

Has Abstract

pub_date

2002-09-25 00:00:00

pages

177-82

issue

1-3

eissn

0014-5793

issn

1873-3468

pii

S0014579302032957

journal_volume

528

pub_type

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