Patch-clamp electrical recordings of rutaecarpine-induced block of delayed rectifier K current in NG-108-15 neuronal cells

by Lin, Pei-Hsuan

Abstract (Summary)
Abstract In the present study, the effects of rutaecarpine on ionic currents of NG108-15 neuronal cells were studied. Rutaecarpine (2-100 £gM) suppressed the amplitude of voltage-dependent K+ outward current (IK(DR)) in a concentration-dependent manner. The IC50 value for rutaecarpine-induced inhibition of IK was 11£gM. However, rutaecarpine (20 £gM) had little effect on L-type Ca2+ current. IK(DR) present in these cells is sensitive to the inhibition by quinidine and dendrotoxin, yet not by E-4031. Rutaecarpine enhanced the rate and extent of IK(DR) inactivation, although it had no effect on the initial activation phase of IK(DR). Recovery from block by rutaecarpine (5 £gM) was fitted by a single exponential with a value of 2.87 s. Cell-attached single-channel recordings revealed that rutaecarpine decreased channel activity over the length of the test potential without altering single-channel amplitude. With the aid of binding scheme, a quantitative description of the actions of rutaecarpine on IK(DR) was provided. Under current-clamp configuration, rutaecarpine also prolonged action potential duration in NG108-15 cells without altering other variables of the action potential. The results clearly show that rutaecarpine is a blocker of the KDR channel. The increase in action potential duration induced by rutaecarpine can be explained mainly by its blocking effects on IK(DR).
Bibliographical Information:

Advisor:Chung-Ren Jan; Sheng-Nan Wu; Hung-Tu Huang

School:National Sun Yat-Sen University

School Location:China - Taiwan

Source Type:Master's Thesis

Keywords:rutaecarpine patch clamp


Date of Publication:07/04/2002

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