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001-es BibID:BIBFORM006036
Első szerző:Gáspár Rezső (biofizikus)
Cím:Effects of bretylium tosylate on voltage-gated potassium channels in human T lymphocytes / Gaspar, R., Panyi, G., Ypey, D. L., Krasznai, Z., Vereb, G., Pieri, C., Damjanovich, S.
Dátum:1994
Megjegyzések:Using the patch-clamp technique, we determined that bretylium tosylate, a quaternary ammonium compound possessing immunomodulating activity, decreased the whole-cell K+ current in human T lymphocytes, in a dose-dependent manner, in the 0.05-5 mM extracellular concentration range. Bretylium tosylate prolonged the recovery from inactivation and accelerated the inactivation and deactivation of the K+ current but did not influence the kinetics of activation or the voltage dependence of activation and steady state inactivation of the K+ conductance. The percentage of drug-induced block was independent of membrane potential. K+ channel block by bretylium tosylate was partially and slowly removable by washing with drug-free extracellular solution. Bovine serum albumin (10 mg/ml) in the bath lifted the drug-induced block almost instantaneously, although not completely. In control experiments bovine serum albumin increased the inactivation time constant of the K+ channels but left the peak K+ current amplitude unaffected. On the basis of the experimental evidence, a gating-dependent allosteric interaction is suggested for the mechanism of drug action. The effective dose range, time of exposure, and reversibility of bretylium tosylate-induced K+ channel block correlated well with the same parameters of the drug-induced inhibition of T lymphocyte activation. The reported effects of bretylium tosylate on T cell mitogenesis can be regarded partly as a consequence of its blocking effects on voltage-gated K+ channels.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Bretylium Tosylate
Cell Membrane
drug effects
Electrophysiology
Human
Hungary
In Vitro
Ion Channel Gating
Kinetics
Lymphocytes
pharmacology
physiology
Potassium
Potassium Channels
Support,Non-U.S.Gov't
T-Lymphocytes
Megjelenés:Molecular pharmacology. - 46 : 4 (1994), p. 762-766. -
További szerzők:Panyi György (1966-) (biofizikus) Ypey, Dirk L. Krasznai Zoltán (1950-) (biofizikus) Vereb György (1965-) (biofizikus, orvos) Pieri, Carlo Damjanovich Sándor (1936-2017) (biofizikus)
Internet cím:elektronikus változat
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