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Interaction of the Novel Anticonvulsant, BIA 2‐093, with Voltage‐Gated Sodium Channels: Comparison with Carbamazepine by M. J. Bonifácio; R. D. Sheridan; A. Parada; R. A. Cunha; L. Patmore; P. Soares‐da‐Silva is a Medicine article available to read on EtoBox.

What is Interaction of the Novel Anticonvulsant, BIA 2‐093, with Voltage‐Gated Sodium Channels: Comparison with Carbamazepine about?

**Summary:** **Purpose:** BIA 2‐093 [(__S__)‐(‐)‐10‐acetoxy‐10,11‐dihydro‐5H‐dibenz/b,f/azepine‐5‐carboxamide] is endowed with an anticonvulsant potency similar to that of carbamazepine (CBZ), but produces less cognitive and motor impairment. This study evaluated whether voltage‐gated sodium channels (VGSCs) are a primary locus for the action of BIA 2‐093. **Methods:** We used the whole‐cell voltage‐clamp technique in the mouse neuroblastoma cell line N1E‐115 to investigate the effects of BIA 2‐093 and CBZ on VGSCs, displacement of [^3^H]‐batrachotoxinin A 20‐α‐benzoate ([^3^H]‐BTX), and [^3^H]‐saxitoxin to define their relative potency to bind to rat brain sodium channels, and inhibition of uptake of ^22^Na by rat brain cortical synaptosomes stimulated by veratridine as a measure of sodium entry. **Results:** The inhibitory potencies of BIA 2‐093 and CBZ increased as the holding potential was made less negative (−100, −90, −80, and −70 mV) with median inhibitory concentration (IC~50~) values (in μ__M__) of, respectively, 4,337, 618, 238, and 139 for BIA 2‐093, and 1,506, 594, 194, and 101 for CBZ. BIA 2‐093 displayed a similar potency in displacing [^3^H]‐BTX (IC~50~ values, 222

Who reads Interaction of the Novel Anticonvulsant, BIA 2‐093, with Voltage‐Gated Sodium Channels: Comparison with Carbamazepine?

Author

M. J. Bonifácio; R. D. Sheridan; A. Parada; R. A. Cunha; L. Patmore; P. Soares‐da‐Silva

Publisher

Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0013-9580)

Published

2001

Language

EN

Field

Medicine (Health Sciences)