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Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.

Abstract：

: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 sigma1 binding. Both anticonvulsant and Na+ channel blocking activities were independent of stereochemistry, while sigma1 binding seems to be favoured by an S-configuration on the aminoamide moiety.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Pevarello P,Bonsignori A,Caccia C,Amici R,McArthur RA,Fariello RG,Salvati P,Varasi M

doi

10.1016/s0960-894x(99)00415-1

subject

Has Abstract

pub_date

1999-09-06 00:00:00

pages

2521-4

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960894X99004151

journal_volume

9

pub_type

杂志文章

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