Competition for binding between veratridine and KIFMK: an open channel blocking peptide of the RIIA sodium channel

Ghatpande, A. S. ; Sikdar, S. K. (1997) Competition for binding between veratridine and KIFMK: an open channel blocking peptide of the RIIA sodium channel Journal of Membrane Biology, 160 (3). pp. 177-182. ISSN 0022-2631

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Official URL: http://www.springerlink.com/content/r6yjmnpldqx00l...

Related URL: http://dx.doi.org/10.1007/s002329900306

Abstract

Veratridine, an alkaloid isolated from the rhizome of V. album, binds and slows the inactivation of the brain sodium channels. The synthetic pentapeptide KIFMK causes a voltage- and use-dependent open-channel block of the RIIA (rat brain type IIA) sodium channel (Eaholtz, Scheuer & Catterall, 1994). Our studies on the RIIA sodium channel expressed in CHO cells reveal that the fraction of veratridine modified sodium channels decreases linearly with increasing KIFMK concentration. However, the time constant for dissociation of veratridine from the channel remains unchanged in the presence of a high concentration of KIFMK, as opposed to that in the presence of QX314 where the dissociation appears to be more complex. These data are consistent with mutually exclusive binding of the open channel blocking peptide and veratridine to the brain sodium channel.

Item Type:Article
Source:Copyright of this article belongs to Springer.
Keywords:Veratridine; KIFMK; Sodium Channel; Binding Competition; Site 2 Receptor; Whole Cell Patch Clamp
ID Code:90206
Deposited On:07 May 2012 13:26
Last Modified:07 May 2012 13:26

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