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001-es BibID:BIBFORM004653
035-os BibID:(PMID)10368833
Első szerző:Varga E.
Cím:Nonspecific membrane effects of CH-103 : hydrophobicity, surface activity and membrane fluidity studies in comparison with propranolol and practolol / Varga, E., Szollosi, J., Antal, K., Kovacs, P., Szabo, J. Z.
Dátum:1999
Megjegyzések:The partition coefficient, surface activity and membrane fluidizing/disordering effects of CH-103, a beta-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+, Mg(2+)-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.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
Adrenergic beta-Antagonists
Amino Alcohols
Animal
Cattle
Chemistry, Physical
Comparative Study
cytology
drug effects
Fluorescence
Fluorescence Polarization
Hungary
In Vitro
Male
Membrane Fluidity
pharmacology
Practolol
Propranolol
Semen
Surface Properties
Surface Tension
Megjelenés:Die Pharmazie. - 54 : 5 (1999), p. 380-384. -
További szerzők:Szöllősi János (1953-) (biofizikus) Antal Károly (1956-) (kémikus) Kovács P. Szabó Judit Zsuzsanna (farmakológus, klinikai laboratóriumi szakorvos)
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