Is bupivacaine a decoupler, a protonophore or a proton‐leak‐inducer?

FEBS Letters

Schönfeld, P.¹  Dabadie, P.²  Slimani, M.³  Mazat, J.-P.³  Sztark, F.² 

[1] Medizinische Akademie Magdeburg, Institut für Biochemie, Leipziger Strasse 44, 3090 Magdeburg, Germany;Département d'Anesthésie-Réanimation Hôpital Pellegrin, 146 Rue Léo Saignat, 33076 Bordeaux Cedex, France;Université Bordeaux II, 146 Rue Léo Saignat, 33076 Bordeaux Cedex, France

关键词: Local anesthetic;    Bupivacaine;    Uncoupling;    Mitochondria;    Rat heart;    CCCP;    carbonylcyanide m-chlorophenylhydrazone;    TPB−;    tetraphenylboron;    VAL;    valinomycin;    BUPI;    bupivacaine;    1-butyl-N-(2;    6-dimethylphenyl)-2-piperidinecarboxamide;    QX 572;    dimethyldiphenyl-acetamido-ammonium;    BCECF/AM;    acetoxymethyl ester of 2;    7-biscarboxy-ethyl-5(6)-carboxyfluorescein;    TPP+;    tetraphenylphosphonium;    RHM;    rat-heart mitochondria;   

DOI  :  10.1016/0014-5793(92)80636-U

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

This paper deals with the mechanism of bupivacaine uncoupling of oxidative phosphorylation in rat heart mitochondria. By comparison with the effects of QX 572, a permanently charged quarternary amine-type local anesthetic, it is concluded that the effects of bupivacaine and QX 572 may be explained by classical uncoupling behaviour. In the case of bupivacaine this uncoupling effect is mediated through a protonophore-like mechanism, whereas that of QX 572 is simply explained by an electrophoretic uptake.

【 授权许可】

Unknown