Document Detail

Uptake of chloroquine by human erythrocytes.
MedLine Citation:
PMID:  2306282     Owner:  NLM     Status:  MEDLINE    
Analysis of studies of the pH dependence of the kinetics of chloroquine (CQ) uptake by human erythrocytes indicates that the unionised CQ species is the major membrane permeant at physiological pH even though the concentration of this species as a fraction of the total CQ concentration in solution is extremely small (0.01% at pH 7.4). CQ concentration-dependence studies and studies performed in the presence of various substrates and inhibitors of erythrocyte membrane transport failed to provide evidence of saturation or inhibition of CQ transport, which suggests that the likely mechanism of CQ transport across human erythrocyte membranes is by passive diffusion. Results of equilibrium binding studies of CQ to intact and lysed human erythrocytes indicated that the mechanism of CQ accumulation in intact human erythrocytes appears to be by a combination of ion trapping (a consequence of the basic nature of the drug and the pH gradient across the human erythrocyte membrane) and binding of CQ to cell components.
V Ferrari; D J Cutler
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Biochemical pharmacology     Volume:  39     ISSN:  0006-2952     ISO Abbreviation:  Biochem. Pharmacol.     Publication Date:  1990 Feb 
Date Detail:
Created Date:  1990-03-26     Completed Date:  1990-03-26     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0101032     Medline TA:  Biochem Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  753-62     Citation Subset:  IM    
Department of Pharmacy, University of Sydney, NSW, Australia.
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MeSH Terms
4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid
4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic Acid / analogs & derivatives,  pharmacology
Amino Acids / blood
Biological Transport / drug effects
Blood Glucose / metabolism
Carrier Proteins / blood
Chloroquine / blood*
Choline / blood
Erythrocyte Membrane / metabolism
Erythrocytes / metabolism*
Hydrogen-Ion Concentration
Membrane Potentials
Nucleosides / blood
Verapamil / pharmacology
Reg. No./Substance:
0/Amino Acids; 0/Blood Glucose; 0/Carrier Proteins; 0/Nucleosides; 27816-59-7/4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic Acid; 52-53-9/Verapamil; 53005-05-3/4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid; 54-05-7/Chloroquine; 62-49-7/Choline

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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