Local anesthetics: a new class of partial inhibitors of mitochondrial ATPase.
The following characteristics are reported for mitochondrial ATPase prepared by the chloroform extraction method: (1) The pH optimum for enzyme activity is at 8.0. (2) The neutral anesthetic benzocaine inhibits the enzyme at all pH values. (3) Reciprocal plots of 1/v versus 1/[ATP] show that inhibition by lidocaine, tetracaine, dibucaine, and chlorpromazine is noncompetitive; slope and intercept replots are hyperbolic, showing that the inhibition is partial rather than complete.
D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D002417:Cattle; D002746:Chlorpromazine / Q000494:pharmacology; D003992:Dibucaine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008012:Lidocaine / Q000494:pharmacology; D008274:Magnesium / Q000502:physiology; D008929:Mitochondria, Heart / Q000201:enzymology; D006180:Proton-Translocating ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013748:Tetracaine / Q000494:pharmacology
D000779:Anesthetics, Local; D013748:Tetracaine; D008012:Lidocaine; D006180:Proton-Translocating ATPases; D008274:Magnesium; D003992:Dibucaine; D002746:Chlorpromazine