Calcium level controlling activities of novel derivatives of amlodipine, riodipine and cerebrocrast

R. Vilskersts, B. Vigante, Z. Neidere, A. Krauze, I. Domracheva, L. Bekere, I. Shestakova, G. Duburs, M. Dambrova

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC 50=39 μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC 50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.

Original languageEnglish
Pages (from-to)322-328
Number of pages7
JournalLetters in Drug Design and Discovery
Volume9
Issue number3
DOIs
Publication statusPublished - Mar 2012
Externally publishedYes

Keywords

  • Amlodipine
  • Asymmetric 1,4-dihydropyridines
  • Calcium channel antagonists
  • Cerebrocrast
  • Riodipine

Field of Science

  • 3.1 Basic medicine

Publication Type

  • 1.1. Scientific article indexed in Web of Science and/or Scopus database

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