Uncoupling effects of local anesthetics on rat liver mitochondria.
We demonstrate in this paper that bupivacaine, a local anesthetic, can act alone as an uncoupler of rat liver mitochondria. It stimulates state 4 respiration, induces a swelling in potassium acetate (in the presence of valinomycin), and collapses the transmembrane potential. Lidocaine, another local anesthetic, requires the presence of a lipophilic anion such as TPB- to produce the same effects. TPB- can also reinforce the action of bupivacaine. These differences in action of the two local anesthetics can be explained by the difference in the liposolubility.
Université Bordeaux II, CNRS, Bordeaux, France.
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Dabadie
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Bendriss
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Erny
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Mazat
D000818:Animals; D002045:Bupivacaine / Q000494:pharmacology*; D002258:Carbonyl Cyanide m-Chlorophenyl Hydrazone / Q000494:pharmacology; D007425:Intracellular Membranes / Q000187:drug effects / Q000502:physiology; D007700:Kinetics; D008012:Lidocaine / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects; D008930:Mitochondria, Liver / Q000187:drug effects / Q000378:metabolism*; D008933:Mitochondrial Swelling / Q000187:drug effects; D010101:Oxygen Consumption / Q000187:drug effects*; D051381:Rats; D011919:Rats, Inbred Strains; D014475:Uncoupling Agents; D014634:Valinomycin / Q000494:pharmacology
D014475:Uncoupling Agents; D014634:Valinomycin; D002258:Carbonyl Cyanide m-Chlorophenyl Hydrazone; D008012:Lidocaine; D002045:Bupivacaine