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Incorporation of reserpine into isolated rat peritoneal mast cells and mast cell granules in vitro.

1972; National Institutes of Health; Volume: 86; Issue: 4 Linguagem: Inglês

J. Gripenberg,

Synthesis and Catalytic Reactions

The incorporation of guanethidine into isolated rat peritoneal mast cells was studied in vitro. The incorporation of the drug is dependent upon 1. temperature, 2. the pH of the medium, 3. the presence of Ca-ions in the medium, it 4. shows saturation characteristics and is 5. inhibited by 5-hydroxytryptamine and tricyclic antidepressants. Of the metabolic inhibitors tested, only FCCP reduced incorporation of guanethidine. The intracellular location of guanethidine in mast cells is mainly in the amine-storing organelles. It is concluded that the incorporation of guanethidine is partly due to an active transport mechanism located in the cell membrane, while the incorporation of the drug into isolated membrane-free mast cell granules is a passive process resulting in binding to sites in the granule matrix.