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Long‐term regulation of voltage‐gated Ca 2+ channels by gabapentin
Author(s) -
Kang Myoung-Goo,
Felix Ricardo,
Campbell Kevin P
Publication year - 2002
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(02)03295-7
Subject(s) - xenopus , protein subunit , gabapentin , chemistry , biophysics , recombinant dna , kinetics , biochemistry , biology , medicine , physics , alternative medicine , pathology , quantum mechanics , gene
Gabapentin (GBP) is a γ‐aminobutyric acid analog effective in the treatment of seizures. A high‐affinity interaction between GBP and the α 2 δ 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.