Bepridil inhibition of sodium current in rat hippocampal CA1 neurons.
OBJECTIVE
To study the effects of bepridil on sodium current in rat hippocampal neurons.


METHODS
All experiments were performed on acutely isolated hippocampal pyramidal neurons by means of whole-cell patch-clamp techniques. Recording media contained ion channel blockers to allow the selective activation of voltage-dependent sodium currents.


RESULTS
Bepridil reduced the amplitudes of sodium current in time- and concentration-dependent manners. The half-blocking time was about 10 min in bepridil 10 micromol.L-1, and IC50 was 2.6 (2.3-2.9) micromol.L-1. Bepridil 10 micromol.L-1 shifted the maximal activation of sodium current from -50 mV to -40 mV, and the characteristic voltage of inactivation from -71 mV to -89 mV without changing the slope factor.


CONCLUSIONS
Bepridil blocked voltage-dependent sodium current of hippocampal CA1 neurons and might have therapeutic actions for ischemia-induced brain damage.
Department of Pharmacology of Chinese Materia Medica, China Pharmaceutical University, Nanjing 210009, China.
H J
HJ
Hu
D M
DM
Yang
D Z
DZ
Dai
C H
CH
Wu
P A
PA
Zhou
D000818:Animals; D015764:Bepridil / Q000494:pharmacology*; D005260:Female; D008297:Male; D009474:Neurons / Q000502:physiology; D018408:Patch-Clamp Techniques; D017966:Pyramidal Cells / Q000502:physiology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D015222:Sodium Channels / Q000187:drug effects*
D015222:Sodium Channels; D015764:Bepridil