Membrane-altering effects of velnacrine and N-methylacridinium: Relevance to tacrine and Alzheimer's disease

D. Allan Butterfield, Anuradha Rangachari

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

The interaction of pharmacological agents potentially useful in Alzheimer's disease, 9-amino-1,2,3,4-tetrahydroacridine (THA or tacrine) and its major metabolite velnacrine (or HP-029), along with related compounds with cytoskeletal proteins in human erythrocyte membrane was investigated using electron paramagnetic resonance spin labeling techniques. The results suggest that: (1) the position of the positive charge of tacrine may be important in the mechanism of its interaction with the membrane cytoskeleton; (2) like tacrine, velnacrine also strengthens cytoskeletal protein-protein interactions in erythrocyte membranes, but appears to be only about half as potent as tacrine. These results are discussed with relevance to therapeutic use of these agents in Alzheimer's disease.

Original languageEnglish
Pages (from-to)596-603
Number of pages8
JournalBiochemical and Biophysical Research Communications
Volume185
Issue number2
DOIs
StatePublished - Jun 15 1992

Bibliographical note

Funding Information:
This work was supported in part by grants from the National Science Foundation (RII-86-10671; EHR-9108764). We thank Hoechst-Roussel Pharmaceuticals, Inc. for their generous gift of HP-029 and HP-5950.

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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