Permeability of Erythrocyte Membrane to Organic Mercurials

概要

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Permeability of erythrocyte membrane to PCMBS (parachloromercuriphenyl sulfonic acid), PCMB (parachloromercuribenzoic acid) and chlormerodrin (a mercurial diuretic) was investigated by using radioactive 203Hg compounds. Among these three mercurials, the rate of uptake was in the order of PCMBS<chlormerodrin<PCMB. SITS (4-acetamido 4'-isothiocyanostilbene-2, 2'-disulfonic acid) which modifies amino groups in erythrocytes membrane inhibited PCMBS uptake, while permeability of PCMB and chlormerodrin was not affected. The effect of SITS on PCMBS permeability was decreased in a lower temperature. The activation energy of PCMBS uptake was 21.1kcal/mole, and at least two kinds of activation energy (22.7 and 10.2kcal/mole) were determined in the presence of SITS. Superficial binding of PCMBS to red cell membrane was markedly eliminated by PCMB, while the rate of uptake of PCMBS was not affected. The PCMB uptake was accelerated at a lower pH. The optimum pH for uptake of PCMBS was shown to be a 7, which was lowered in the presence of SITS. On the basis of these results, at least two pathways can be differenciated. One is the aqueous pathway for anionic substances such as PCMBS, which is inhibited by SITS and related to K+ permeability. The other is in lipid nature and provides rapid penetration for non-ionic reagents.
Japan Society of Clinical Chemistryの論文