Journal
PHARMACOLOGICAL RESEARCH
Volume 43, Issue 4, Pages 399-403Publisher
ACADEMIC PRESS LTD
DOI: 10.1006/phrs.2001.0803
Keywords
local anesthetics; Na+; K+-ATPase; enzyme inhibition; lidocaine; procaine; chloroprocaine; bupivacaine; mepivacaine; quaternary amines; QX-222; QX-314
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Funding
- NIGMS NIH HHS [R01 GM50764] Funding Source: Medline
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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 degreesC. Chloroprocaine (IC50 = 13 mM) had slightly greater potency than procaine (IC50 = 17.7 mM). Bupivacaine (IC50 = 6.7 mM) was more potent than its congener mepivacaine (IC50 > 10 mM, the solubility limit). QX-222 (IC50 > 600 mM) and QX-314 (IC50 = 132 mM) had less potency than lidocaine (IC50 = 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. (C) 2001 Academic Press.
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