title: The intracellular sodium activity of sheep heart Purkinje fibres: effects of local anaesthetics and tetrodotoxin.
abstract: 1. The intracellular Na activity (a(Na) (i)) of quiescent sheep heart Purkinje fibres has been measured using Na(+)-sensitive glass micro-electrodes. The effects of local anaesthetics (procaine and lidocaine) and tetrodotoxin (TTX) have been investigated.2. Local anaesthetics reduced the steady-state level of the intracellular Na activity in a dose-dependent manner. The highest concentrations used (10(-2)M) reduced the intracellular Na activity by about 25%.3. TTX decreased the steady-state level of the intracellular Na activity. At a concentration of 10(-6) g/ml. (3.13 x 10(-6)M), TTX produced a decrease in intracellular Na activity of approximately 10%.4. The initial rate of rise of the intracellular Na activity upon addition of the cardioactive steroid strophanthidin (10(-5)M) was used to estimate the net passive Na influx.5. Procaine (5 x 10(-4)M) caused a 50% reduction of this rate of rise of the intracellular Na activity. The highest concentration of procaine used (10(-2)M) decreased the rate of rise by approximately 80%.6. Procaine (5 x 10(-3)M) also reduced the rate of rise of intracellular Na produced by the removal of external K (K(o)), and prevented the large depolarization associated with the absence of K(o).7. TTX also produced a decrease in the rate of rise of the intracellular Na activity that occurs upon addition of strophanthidin. A maximum effect was produced in our experiments at a TTX concentration of 10(-6) g/ml. At this concentration the rate of rise of intracellular Na activity was reduced by approximately 40% at a membrane potential of -70 mV.8. We conclude from our experiments that the effects of local anaesthetics and TTX on the intracellular Na activity are brought about by a reduction of the Na permeability of the cell membrane, and that at the normal resting potential, Na entry through TTX-sensitive channels contributes greatly to the total net Na influx.
mesh_terms: D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002463:Cell Membrane Permeability / Q000187:drug effects; D006329:Heart Conduction System / Q000502:physiology*; D066298:In Vitro Techniques; D007424:Intracellular Fluid / Q000502:physiology; D008012:Lidocaine / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects; D011343:Procaine / Q000494:pharmacology*; D011690:Purkinje Fibers / Q000187:drug effects / Q000378:metabolism / Q000502:physiology*; D012756:Sheep; D012964:Sodium / Q000378:metabolism / Q000502:physiology*; D013327:Strophanthidin / Q000494:pharmacology; D013779:Tetrodotoxin / Q000494:pharmacology*
chemical_list: D013779:Tetrodotoxin; D011343:Procaine; D013327:Strophanthidin; D008012:Lidocaine; D012964:Sodium