Advanced search×

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
Version: za2963e q8zaa q8zb8 q8zc6 q8zdc q8ze2 q8zfd q8zg6

Similar articles you may find interesting…

  1. Investigation of mercury methylation pathways in biofilm versus planktonic cultures of Desulfovibrio desulfuricans.
    Tiffany Y Lin, Rita Ann Kampalath, and Jennifer Ayla Jay

    Environ Sci Technol (2013) PMID 23634937

    Our previous study showed that methylation rates in biofilm cultures were up to an order of magnitude greater than those in planktonic cultures of a sulfate-reducing bacterium. To probe whether the differential Hg methylation rates resulted from metabolic differences between these two cultures, Hg m...
  2. High-level expression and efficient one-step chromatographic purification of a soluble human leukemia inhibitory factor (LIF) in Escherichia...
    Keitaro Imaizumi, Shin-Ichi Nishikawa, and Teruo Akuta

    Protein Expr Purif (2013) PMID 23628981

    We present the high level expression of a soluble recombinant human LIF (rhLIF) in Escherichia coli. A codon-optimized Profinity eXact(TM)-tagged hLIF cDNA was cloned into pET3b vector, and transformed into Escherichia coli OrigamiB(DE3) harboring the bacterial thioredoxin coexpression vector. By us...
  3. In Vitro Evaluation of Combined Sulfated Silk Fibroin Scaffolds for Vascular Cell Growth.
    Haifeng Liu, Xili Ding, and Yubo Fan

    Macromol Biosci (2013) PMID 23610045

    A combined sulfated silk fibroin scaffold is fabricated by modifying a knitted silk scaffold with sulfated silk fibroin sponges. In vitro hemocompatibility evaluation reveals that the combined sulfated silk fibroin scaffolds reduce platelet adhesion and activation, and prolong the ac...