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Journal of Pharmacology And Experimental Therapeutics, Vol. 133, Issue 3, 325-331, 1961
Copyright © 1961 by American Society for Pharmacology and Experimental Therapeutics

PASSAGE OF ORGANIC BASES INTO HUMAN RED CELLS

Lewis S. Schanker 1, Panayotis A. Nafpliotis 1, and Jean M. Johnson 1

1 Laboratory of Chemical Pharmacology, National Heart Institute, Bethesda, Maryland

The rates at which 14 organic bases enter the human red cell in vitro are related to the lipid/water partition coefficients of the compounds—the higher the coefficient the greater the rate of entry. The degree of ionization of the compounds is also important in determining the rate of entry, but mainly because it defines the proportion of drug in the lipid-soluble (undissociated) form. The results support the view that the erythrocyte membrane behaves as a lipid-like barrier to the penetration of organic compounds.

The degree of intracellular binding of drugs has been estimated from the binding to suspensions of broken red cells. The intracellular binding of serotonin and p-nitroaniline is largely accounted for as binding to hemoglobin.

Submitted on March 1, 1961




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Copyright © 1961 by the American Society for Pharmacology and Experimental Therapeutics.