Inhibition of cytochrome oxidase activity by local anaesthetics

• Published in: Biochemical pharmacology Vol. 32; no. 18; p. 2715
• Main Authors: Casanovas, A M, Malmary Nebot, M F, Courrière, P, Oustrin, J
• Format: Journal Article
• Language: English
• Published: England 15-09-1983
• Subjects: Anesthetics, Local - pharmacology; Binding, Competitive; Electron Transport Complex IV - antagonists & inhibitors; Kinetics; Polarography; Structure-Activity Relationship
• ISSN: 0006-2952
• DOI: 10.1016/0006-2952(83)90081-3

Using a polarographic method, we studied the inhibition of mitochondrial electron transport at the cytochrome c oxidase site caused by eight local anaesthetics. The diversity of the types of inhibition observed indicate the importance of electrostatic interactions between the anaesthetic molecules and the membrane protein. A linear relationship was recognized between the anaesthetic activity of infiltration and the affinity for the enzyme. We also observed a significant relationship between this affinity and the octanol-water partition coefficient. This result suggests that lipophilic interactions are involved in cytochrome oxidase-anaesthetic binding. We tried to establish a parallel between this binding and the mechanism of anaesthesia involving the nerve membrane proteins.