The use of spin labeling techniques in studies on the effects of drugs on membranes was reviewed and discussed. An example of the clinical application of this technique would be in the determination of the clinical concentration of the inhalation anesthetic halothane (151677) needed to make a large change in the outer and inner hyperfine extrema. Pitfalls in the use of spin labeling for the measurement of changes in the dynamics or structures of membranes were noted, and assumptions made in the process were discussed. The phase transitions and phase separations in membranes, and the partitioning of the spin label 2,2,6,6-tetramethylpiperidine-N-oxyl (TEMPO) were described. Topics discussed under pH and electrostatic gradients across membranes included measurement by phosphonium spin labels, and the effects of drugs on gradients. The author concludes that it is likely that new ESR techniques will become very useful in the study of the effects of drugs on membranes; these techniques allow static as well as kinetic data on ion flow through membranes, and make possible definition of the contributions of entropy and enthalpy to the thermodynamic forces that govern ion movement.
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