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

D. Allan Butterfield; Anuradha Rangachari

doi:10.1016/0006-291X(92)91666-E

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

D. Allan Butterfield
, Anuradha Rangachari

Producción científica: Article › revisión exhaustiva

10 Citas (Scopus)

Resumen

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.

Idioma original	English
Páginas (desde-hasta)	596-603
Número de páginas	8
Publicación	Biochemical and Biophysical Research Communications
Volumen	185
N.º	2
DOI	https://doi.org/10.1016/0006-291X(92)91666-E
Estado	Published - jun 15 1992

Nota bibliográfica

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.

Financiación

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.

Financiadores	Número del financiador
National Science Foundation (NSF)	RII-86-10671, EHR-9108764

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

Good health and well being

ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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10.1016/0006-291X(92)91666-E

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

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.",

author = "Butterfield, \{D. Allan\} and Anuradha Rangachari",

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.",

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AU - Butterfield, D. Allan

AU - Rangachari, Anuradha

N1 - 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.

PY - 1992/6/15

Y1 - 1992/6/15

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AB - 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.

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

Resumen

Nota bibliográfica

Financiación

ODS de las Naciones Unidas

ASJC Scopus subject areas

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