Tamura Akira

Shape changes of human erythrocytes induced by various amphipathic drugs acting on the membrane of the intact cells.

Abstract Most of the amphipathic drugs acting on nerves (general and local anesthetics, neuroleptics. antipyretics-analgesics, non-steroidal anti-inflammatory agents, etc.) and some other drugs (anti-histaminic agents, plant alkaloids, etc.) were found to induce instantly one of two typical types of shape changes of human erythrocytes when added into the cell suspension. It was confirmed that, generally, drugs with an anionic polar group induced membrane externalization (crenation), and those with a cationic group induced membrane internalization (invagination). The drugs in the former group are antagonistic against the shape-transforming effects of the drugs in the latter group, and vice versa. Drugs with a neutral polar group or with a quarternary ammonium group induced a complex type of shape change, suggesting the intramembraneous translocation of these drugs.