Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants

Paolo Pevarello, Alberto Bonsignori, Carla Caccia, Raffaella Amici, Robert A. McArthur, Ruggero G. Fariello, Patricia Salvati, Mario Varasi

Research output: Contribution to journalArticle

Abstract

Sodium channel blocking, anticonvulsant activity, and sigma (σ) binding of selected leads in a series of α-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 σ1 binding. Both anticonvulsant and Na+ channel blocking activities were independent of stereochemistry, while σ1 binding seems to be favoured by an S-configuration on the aminoamide moiety.

Original languageEnglish
Pages (from-to)2521-2524
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume9
Issue number17
DOIs
Publication statusPublished - Sep 6 1999

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Keywords

  • Anticonvulsants
  • Neurologically active compds
  • Sigma receptors
  • Sodium channel

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Pevarello, P., Bonsignori, A., Caccia, C., Amici, R., McArthur, R. A., Fariello, R. G., Salvati, P., & Varasi, M. (1999). Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants. Bioorganic and Medicinal Chemistry Letters, 9(17), 2521-2524. https://doi.org/10.1016/S0960-894X(99)00415-1