Perturbation effect of eight calcium channel blockers on liposomal membranes prepared from rat brain total lipids.
EPR spectroscopy of phosphatidylcholine or stearic acid labeled at the doxyl group at the 16-carbon position was used to compare the perturbation effect of eight calcium channel blockers (CB) on overall dynamics/disorder of the hydrophobic part of liposome membranes prepared from rat brain total lipids at the drug/lipid molar ratio of 1/2. Nifedipine (NIF), nimodipine, niludipine and nitrendipine had a minor effect on the dynamics/disorder of the liposome membranes, whereas the disordering effect of verapamil (VER), mepamil, gallopamil and diltiazem was more pronounced. Concentration dependence of the overall disordering effect of VER on liposomal membranes was found at the VER/lipid ratio greater than 0.02 and for the tranquilizer thioridazine greater than 0.005. VER exerted a disordering effect at the hydrophobic part of synaptosomal membranes at concentrations greater than or equal to 0.32 mmol/l, whereas NIF did not exhibit a disordering effect even at concentrations of 10-20 mmol/l.
Ondrias
K
K
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, CSFR.
Ondriasová
E
E
Stasko
A
A
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D004578:Electron Spin Resonance Spectroscopy; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000378:metabolism*; D008566:Membranes / Q000187:drug effects; D015394:Molecular Structure; D051381:Rats; D013574:Synaptosomes / Q000187:drug effects*; D014700:Verapamil / Q000494:pharmacology
D002121:Calcium Channel Blockers; D008055:Lipids; D008081:Liposomes; D014700:Verapamil