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 Lettjournal_title
FEBS lettersauthors
Kang MG,Felix R,Campbell KPdoi
10.1016/s0014-5793(02)03295-7keywords:
subject
Has Abstractpub_date
2002-09-25 00:00:00pages
177-82issue
1-3eissn
0014-5793issn
1873-3468pii
S0014579302032957journal_volume
528pub_type
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