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3@b-hydroxysteroids and pregnenolone sulfate inhibit recombinant rat GABA"A receptor through different channel property

Ming-De Wang, Mozibur Rahman, Di Zhu, Inga-Maj Johansson, and Torbjörn Bäckström

Eur J Pharmacol 557(2-3):8 (2007) PMID 17239367

3@b-hydroxysteroids are pregnenolone sulfate-like GABA"A receptor antagonists. The aim of the current study was to compare the functional differences between 3@b-hydroxysteroids and pregnenolone sulfate to inhibit GABA"A receptors expressed in Xenopus oocytes. Recombinant rat GABA"A receptors encoding wild type @a"1@b"2@c"2"L receptor, mutant @a"1"V"2"5"6"S@b"2@c"2"L and @a"1@b"2"A"2"5"2"S@c"2"L receptors were examined using a two-electrode voltage-clamp technique. A homologous mutation of the residue at 2'position closest to the cytoplasmic end of the M"2 helix to serine on both @a"1 and @b"2 subunit, @a"1"V"2"5"6"S and @b"2"A"2"5"2"S, reduced the slow desensitization components of GABA-activated currents at saturating doses. Compared to the wild type receptor, the potency of GABA increased significantly in the @a"1"V"2"5"6"S@b"2@c"2"L receptor (PA receptor.

Copyright © 2007 Elsevier Ltd. All rights reserved.

DOI: 10.1016/j.ejphar.2006.11.071
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