Binding of the calcium antagonist flunarizine to phosphatidylcholine bilayers : charge effects and thermodynamics

Thomas, P. G. and Seelig, J.. (1993) Binding of the calcium antagonist flunarizine to phosphatidylcholine bilayers : charge effects and thermodynamics. Biochemical Journal, 291 (2). pp. 397-402.

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Official URL: http://edoc.unibas.ch/dok/A5257456

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We have examined the partitioning/transfer of the Ca2+ antagonist flunarizine from the aqueous phase into phospholipid bilayers. We show that the binding of the cationic amphiphilic drug flunarizine to phospholipid bilayers displays traditional linear concentration-dependent characteristics once unmasked of electrostatic effects. The coefficient for the binding/partitioning of flunarizine to phosphatidylcholine was found to be 28700 M-1, supporting the notion that this drug may be particularly membrane-active. The thermodynamics of the partitioning/transfer process have also been studied using high-sensitivity titration calorimetry. Binding was found to be predominantly enthalpy-driven with only a small entropic contribution; delta H = -22.1 kJ.mol-1 (-5.3 kcal.mol-1) at 27 degrees C. This is in conflict with established ideas of entropy-driven partitioning of drugs into phospholipid membranes as a result of the 'hydrophobic effect'. The strong enthalpic nature of binding is interpreted as being indicative of strong lipophilic interactions between the drug and the phospholipid phase.
Faculties and Departments:05 Faculty of Science > Departement Biozentrum > Former Organization Units Biozentrum > Biophysical Chemistry (Seelig J)
UniBasel Contributors:Seelig, Joachim
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Portland Press
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:14 Nov 2017 15:30
Deposited On:22 Mar 2012 13:18

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