PMID: 11900860Mar 20, 2002Paper

BN52021, a platelet activating factor antagonist, is a selective blocker of glycine-gated chloride channel

Neurochemistry International
Elena L KondratskayaO A Krishtal

Abstract

We have found that the platelet activating factor antagonist (BN52021) is an effective blocker of the glycine (Gly) receptor-mediated responses in the hippocampal pyramidal neurons of rat. Using the whole-cell voltage clamp and concentration clamp recording techniques, we investigated the mechanism underlying the inhibitory action of this terpenoid on the glycine-induced chloride current. BN52021 selectively and reversibly inhibits glycine current in a non-competitive and voltage-dependent fashion. The antagonistic effect of this substance is more pronounced at positive membrane potentials. At holding potential -70mV and in the presence of 200 microM glycine IC50 value for the blocking action of BN52021 was 270+/-10nM. Repetitive applications of BN52021 reveal the use-dependence of its blocking action. When co-applied with strychnine (STR), a competitive glycine receptor antagonist, BN52021 does not alter the IC50 value for strychnine. The inhibitory effect of BN52021 on gamma-aminobutyric acid (GABA) current is at least 25 times less potent than the effect on glycine current. This substance fails to affect AMPA and NMDA responses. It may be concluded that BN52021 inhibits glycine-gated Cl- channels by interacting with the pore...Continue Reading

References

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Citations

Oct 22, 2003·Neurochemistry International·Elena L KondratskayaOleg A Krishtal
Apr 22, 2005·Acta Pharmacologica Sinica·Lei ChenJurgen Heschler
Aug 2, 2011·Biological & Pharmaceutical Bulletin·Makoto TsudaKazuhide Inoue
Jun 24, 2004·European Journal of Pharmacology·Shelley H HuangGraham A R Johnston
Aug 30, 2005·Neuropharmacology·Elena L KondratskayaBodo Laube
Jan 29, 2008·Journal of Neurochemistry·Judith A HeadsJoseph W Lynch
Jun 30, 2006·Journal of Neurochemistry·Rebecca HawthorneJoseph W Lynch
Jan 16, 2015·Phytotherapy Research : PTR·Zhixia QiuNing Li
Sep 25, 2003·The Journal of Biological Chemistry·Lidija IvicKristian Strømgaard
Sep 24, 2004·Physiological Reviews·Joseph W Lynch
Nov 16, 2007·Organic & Biomolecular Chemistry·Eisuke KatoKoji Nakanishi
Aug 20, 2005·The Journal of Biological Chemistry·Rebecca Hawthorne, Joseph W Lynch
Oct 4, 2007·The Journal of Biological Chemistry·Stephan A PlessJoseph W Lynch
Jan 1, 2015·SpringerPlus·Galyna MaleevaPiotr Bregestovski
Nov 19, 2015·Frontiers in Molecular Neuroscience·Galyna MaleevaPiotr Bregestovski
Mar 14, 2007·Journal of Medicinal Chemistry·Anders A JensenKristian Strømgaard

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