Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants

被引：26

作者：

Pevarello, P

Bonsignori, A

Caccia, C

Amici, R

McArthur, RA

Fariello, RG

Salvati, P

Varasi, M

机构：

[1] Pharmacia & Upjohn Inc, Dept Chem, I-20014 Milan, Italy

[2] Pharmacia & Upjohn Inc, CNS Biol, I-20014 Milan, Italy

[3] Thomas Jefferson Univ, Dept Neurol, Philadelphia, PA 19107 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期

关键词：

anticonvulsants; neurologically active compds; sodium channel; sigma receptors;

D O I：

10.1016/S0960-894X(99)00415-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Sodium channel blocking, anticonvulsant activity, and sigma (sigma) binding of selected leads in a series of alpha-amino amide anticonvulsants were examined. While anticonvulsant compounds were always endowed with low micromolar sodium (Na+) channel site-2 binding, compounds with low site-2 Na+ channel affinity failed to control seizures. No correlation could be drawn with sigma(1) binding. Both anticonvulsant and Na+ channel blocking activities were independent of stereochemistry, while sigma(1) binding seems to be favoured by an S-configuration on the aminoamide moiety. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2521 / 2524

页数：4

共 22 条

[1]

BENARI Y, 1992, NEUROTRANSMITTERS EP, P369

[2]

CATTERALL WA, 1981, J BIOL CHEM, V256, P8922

[3] Clinical administration of new antiepileptic drugs: An overview of safety and efficacy [J].