Biochemical pharmacology
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Biochemical pharmacology · May 1991
Comparative StudyInhibition of substrate oxidation in mitochondria by the peripheral-type benzodiazepine receptor ligand AHN 086.
The effects, of the benzodiazepines RO5-4864, AHN 086, PK 11195 and clonazepam on respiration of mitochondria from heart, kidney, and liver were studied. ADP-stimulated respiration of heart mitochondria was the most sensitive to inhibition by AHN 086; clonazepam was not inhibitory. Several respiratory chain segment activities of submitochondrial particles were insensitive to AHN 086, except for NADH oxidase which was partially inhibited. ⋯ Phosphate-induced, succinate-dependent swelling was also inhibited by AHN 086 it was not affected by clonazepam. Uncoupled ATP hydrolysis was partially inhibited by RO5-4864, AHN 086, and clonazepam. It is suggested that there is an unspecific inhibition of NADH oxidase and ATP hydrolysis by these benzodiazepines and a specific inhibition on oxidizable substrate transport by the peripheral-type benzodiazepine AHN 086.