On the mechanism of inhibition of the bovine heart F1-ATPase by local anesthetics |
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Authors: | P K Laikind T M Goldenberg W S Allison |
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Institution: | Department of Chemistry, M-001 University of California, San Diego La Jolla, California 92093 USA |
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Abstract: | The rate of inactivation of the mitochondrial F1-ATPase by dicyclohexylcarbodiimide is slowed by concentrations of chlorpromazine, dibucaine, or tetracaine which have been shown by others (B. Chazotte, G. Vanderkooi, and D. Chignell (1982), 310–316) to inhibit the hydrolytic reaction catalyzed by the enzyme. The order of effectiveness of the drugs as protectors of the enzyme against inactivation by dicyclohexylcarbodiimide is: chlorpromazine > dibucaine > tetracaine. Examination of the steady state kinetics showed the chlorpromazine inhibits the ATPase competitively at concentrations up to 18.5 μM while complex kinetic behavior is exhibited at chlorpromazine concentrations from 25–50 μM. These results suggest that the drugs inhibit the F1-ATPase by interacting with the catalytic site of the enzyme and not by promoting its dissociation. |
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Keywords: | DCCD dicyclohexylcarbodiimide |
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