Effects of procaine on intracellular pH and its regulation: measurements with pH-selective micro-electrodes in Retzius neurones of the leech.

The experiments were performed with double-barelled micro-electrodes in Retzius neurones of the leech in order to see if the tertiary amine local anesthetic procaine affects intracellular pH (pHi) and its regulation. Lasting about 20 min, exposures to procaine (3 mM) saline caused an intracellular alkalosis of about 0.2 pH units which gradually degradated; its removal initiated a fast decrease of pHi resulting in an acidosis, fron which the cells recovered. Detailed studies, involving CO2 or NH4+ acid loaded cells as well as inhibition of the pHi regulating exchange mechanism by various drugs or exposures to Na-free salines suggest, that neither the Na+ -H+, nor a probably Na+ -dependent HCO3-(-)Cl- exchange are affected by procaine. We propose a model for procaine action on pHi assuming that neutral procaine passes the membrane easily through lipophilic pathways. The degradation of alkalinity during procaine exposure hints on an entry of loaded procaine, some possible transport paths of which are discussed.