Potassium transport was measured in beta-cell-rich islets from ob/ob-mice using the K+-analogue 86Rb+. Both tetracaine (0.1 mM) and glibenclamide (0.1 microM) reduced the ouabain-resistant 86Rb+ influx but did not significantly affect the ouabain-sensitive portion (Na+/K+ pump). Tetracaine (0.5 - 1 mM) or glibenclamide (0.2 mM) decreased the 86Rb+ equilibrium content and glibenclamide (1 microM) transiently reduced the 86Rb+ efflux rate but 0.1 mM tetracaine had only a slight effect on this flux rate. The results suggest that a change in ouabain-resistant (passive) K+ fluxes, but not the Na+/K+ pump, is involved in stimulation of insulin secretion by glibenclamide and tetracaine. Both drugs may exert similar effects on the beta-cell plasma membrane.
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Eur J Pharmacol
November 1993
Department of Pharmacology, National Defense Medical College, Saitama, Japan.
Effects of local anesthetics and structurally related drugs on the glibenclamide-sensitive K+ currents evoked by Y-26763 (a K+ channel opener) were investigated in native Xenopus oocytes. The K+ current induced by Y-26763 (100 microM) was reversibly suppressed by all six local anesthetics tested in a concentration-dependent manner with the rank order of potencies (IC50 in microM): bupivacaine (67) > dibucaine (136) > tetracaine (845) > lidocaine (1710) = mepivacaine (1945) > procaine (3112). (+)-Propranolol and mexiletine also suppressed Y-26763-induced K+ currents with IC50 values of 115 microM and 789 microM, respectively.
View Article and Find Full Text PDFJ Physiol
February 1987
Department of Pharmacology, University College London.
1. 86Rb and 42K have been used to assess potassium exchange in frog skeletal muscle which had been metabolically exhausted by electrical stimulation (1 Hz) after treatment with 2 mM-cyanide and 1 mM-iodoacetate. These conditions led to the development of rigor.
View Article and Find Full Text PDFActa Physiol Scand
December 1986
Potassium and chloride transport were measured in beta-cell-rich islets from ob/ob-mice using 36Cl- and 86Rb+ (K+-analogue). Reduction of the osmolarity from the normal 317 mosm l-1 to 180 mosm l-1 reduced the apparent content of K+ and Cl-. Hypo-osmolarity had no effect on the ouabain-sensitive portion of the Rb+ influx (Na+/K+ pump), but reduced the ouabain-resistant portion of the influx.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
October 1985
Potassium transport was measured in beta-cell-rich islets from ob/ob-mice using the K+-analogue 86Rb+. Both tetracaine (0.1 mM) and glibenclamide (0.
View Article and Find Full Text PDFThe 45Ca2+ uptake in beta-cell-rich ob/ob-islets was measured using the La3+ wash technique. Tetracaine (1 mM) markedly enhanced the 45Ca2+ net uptake (120 min) in the presence of 3 mM glucose, and at 7 and 20 mM glucose there were clear tendencies to dose-dependent increases with 0.1 to 1 mM tetracaine.
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