1. Academic Validation
  2. Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics

Inhibition of the Na,K-ATPase of canine renal medulla by several local anesthetics

  • Pharmacol Res. 2001 Apr;43(4):399-403. doi: 10.1006/phrs.2001.0803.
H Kutchai 1 L M Geddis
Affiliations

Affiliation

  • 1 Department of Molecular Physiology & Biological Physics, School of Medicine, University of Virginia, Charlottesville, VA 22908, USA. [email protected]
Abstract

The ATPase activity of Na,K-ATPase-enriched membranes from canine renal medulla was determined in the absence of local anesthetic and in the presence of procaine, chloroprocaine, bupivacaine, mepivacaine, lidocaine, and two quaternary derivatives of lidocaine (QX-222 and QX-314) at 37( composite function)C. Chloroprocaine (IC(50)= 13 mM) had slightly greater potency than procaine (IC(50)= 17.7 mM). Bupivacaine (IC(50)= 6.7 mM) was more potent than its congener mepivacaine (IC(50)> 10 mM, the solubility limit). QX-222 (IC(50)> 600 mM) and QX-314 (IC(50)= 132 mM) had less potency than lidocaine (IC(50)= 30.4 mM). This study supports the interpretation that the uncharged forms of local anesthetics are much more potent inhibitors of Na,K-ATPase activity than the cationic forms.

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