The 1,2,3-benzothiadiazoles. A new type of compound acting on coupling site I, in rat liver mitochondria.
1. In rat liver mitochondria, 6-chloro-1,2,3-benzothiadiazole inhibited ADP phosphorylation and Ca2+-transport when the energy required for these processes came from the oxidation of NAD-linked substrates. The inhibition was characterized by substantial reduction in oxygen consumption, H+-movement and disappearance of acceptor control ratio. 2. When the substrate oxidized was succinate, depending on the 6-chloro-1,2,3-benzothiadiazole concn., little or no effect was observed on ADP phosphorylation and Ca2+-transport. 3. The results suggest that 6-chloro-1,2,3-benzothiadiazole can block site I at low concn., but at higher concn. can affect site I and site II, although site I is always more affected.
D000244:Adenosine Diphosphate / Q000378:metabolism; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001693:Biological Transport, Active / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D004140:Dinitrophenols / Q000494:pharmacology; D004734:Energy Metabolism / Q000187:drug effects; D005260:Female; D006859:Hydrogen / Q000378:metabolism; D066298:In Vitro Techniques; D007306:Insecticides / Q000494:pharmacology*; D008930:Mitochondria, Liver / Q000378:metabolism*; D010085:Oxidative Phosphorylation / Q000187:drug effects*; D010101:Oxygen Consumption / Q000187:drug effects; D051381:Rats; D013830:Thiadiazoles / Q000494:pharmacology*
D004140:Dinitrophenols; D007306:Insecticides; D013830:Thiadiazoles; D000244:Adenosine Diphosphate; D006859:Hydrogen; D002118:Calcium