ANTICHOLINESTERASIC DRUGS - TACRINE BUT NOT PHYSOSTIGMINE, ACCUMULATES IN ACIDIC COMPARTMENTS OF THE CELLS

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

卷:1270

Article

DELLATONE, P ; BRAGADIN, M ; ZATTA, P

关键词: TACRINE;    PHYSOSTIGMINE;    LYSOSOME;    THYMOCYTE;    NEUROBLASTOMA CELL;    ALZHEIMERS DISEASE;   

DOI  :  10.1016/0925-4439(94)00079-6

来源: Elsevier

【 摘 要 】

Tacrine (THA) and physostigmine (PHS) have been used in Alzheimer's disease therapy for their anticholinesterasic activity. Here we show that THA is taken up in rat lysosomes in an energy-dependent manner, and that it is also accumulated in acidic compartments of rat thymocytes and neuroblastoma cells. A concentration of THA less than 1 mM dissipated the pH gradient (Delta pH) in all the above mentioned in vitro systems. On the contrary higher concentrations of PHS (1-2 mM) were ineffective. The accumulation of THA in acidic organelles of the cell may be relevant for the pharmacological action of THA in Alzheimer's treatment.

【 授权许可】

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