Nonspecific membrane effects of CH-103: Hydrophobicity, surface activity and membrane fluidity studies in comparison with propranolol and practolol

Edit Varga, J. Szöllosi, K. Antal, P. Kovács, J. Zs Szabó

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Abstract

The partition coefficient, surface activity and membrane fluidizing/disordering effects of CH-103, a β-adrenergic receptor antagonist, were compared to those of propranolol and practolol as reference compounds. Changes in membrane fluidity were followed by measuring the steady-state fluorescence anisotropy of bull sperm cells with 1-[4- (trimethylammonium)phenyl]-6-phenyl-1,3,5-hexatriene(TMA-DPH) as a fluorescence probe. The octanol/buffer (pH 7.0) partition coefficients for CH-103, propranolol and practolol were 32.9, 5.08 and 0.013, respectively; the surface activity of the compounds decreased in the same order. CH-103 and propranolol significantly increased the fluidity of the membrane in a concentration-dependent manner, whereas practolol reduced fluidity. These physicochemical parameters correlated with the effects of these drugs on rat sarcolemmal Ca2+, Mg2+-ATPase, a manifestation of their nonspecific membrane activity. Our results suggest that the physicochemical properties of CH-103, similarly to those of propranolol, are the main determinants of its nonspecific membrane activity.

Original languageEnglish
Pages (from-to)380-384
Number of pages5
JournalPharmazie
Volume54
Issue number5
Publication statusPublished - May 31 1999

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ASJC Scopus subject areas

  • Pharmaceutical Science

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