F020101 | Respiratory states

Compound Dose Time Species Model Method Action Result Positive criterion Reference
Perhexiline 100 μM 5 minutes preincubation mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 193
Amiodarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 4
Perhexiline 200 μM 5 minutes preincubation mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 193
Perhexiline 400 μM 5 minutes preincubation mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 193
Perhexiline 100 μM 5 minutes preincubation mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.05 193
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 4
benzbromarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 4
Pioglitazone decrease Positive 22
Gentamicin 5mM 10min rat isolated rat liver (and kidney) mitochondria Oroboros O2K Oxygraph, complex II-based state 4 respiration increase Positive 316
promethazine increase Positive 22
Gentamicin 5mM 10min rat isolated rat liver mitochondria Oroboros O2K Oxygraph, complex I-based state 4 respiration increase Positive 316
benzbromarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 4
clomipramine decrease Positive 22
Chlorpromazine increase Positive 22
Chlorpromazine decrease Positive 22
imipramine increase Positive 22
Flufenamic Acid 2.9 ± 0.3 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Tolfenamic Acid 3.4 ± 0.6 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Mefenamic acid 17.9 ± 2.2 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Meloxicam 22.8 ± 2.8 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Sudoxicam 37.4 ± 3.0 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Piroxicam 69.0 ± 7.2 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Diflunisal 6.7 ± 1.3 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Diclofenac 56.3 ± 4.9 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Sulindac > 100 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Sulindac sulfide 25.7 ± 4.5 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Nimesulide 2.6 ± 0.2 rat isolated rat liver mitochondria State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive UC50 (nmol/mg mitochondrial protein) 40
Sulindac sulfide 39.8 ± 2.9 rat isolated rat liver mitochondria State 3 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) inhibit Positive IC50 (nmol/mg mitochondrial protein) 40
Miconazole I50=100, 160, 160, 170, 150 μM for substrates Glutamate/Malate, Pyruvate/Malate, Ornithine/Malate, Arginine/Malate and Succinate repectively rat liver mitochondria Clark electrode inhibit Positive 303
clomipramine increase Positive 22
Nimesulide Positive 197
Gentamicin 5mM 10min rat isolated rat liver (and kidney) mitochondria Oroboros O2K Oxygraph, complex II-based state 3u respiration decrease Positive 316
Gentamicin 5mM 10min rat isolated rat liver mitochondria Oroboros O2K Oxygraph, complex I-based state 3u respiration decrease Positive 316
Perhexiline 200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake increase Positive p < 0.01 193
Metformin 2mM 30 minutes mouse; C57BL/6J isolated skeletal muscle mitochondria Measurement of Oxygen level; incubated in complex I substrate; added ADP (500 μM) decrease Positive p < 0.05 172
Metformin 2mM 30 minutes mouse; C57BL/6J isolated skeletal muscle mitochondria Measurement of Oxygen level; incubated in complex I substrate; added oligomycin (2.5 μg oligomycin/mg mitochondrial protein) decrease Positive p < 0.05 172
Nitrofurantoin 1 mM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used glutamate as substrate decrease Positive p < 0.05; 61% inhibition 13
Nitrofurantoin 50 μM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used glutamate as substrate decrease Positive p < 0.05; 72% inhibition 13
Nitrofurantoin 5 μM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used glutamate as substrate decrease Positive p < 0.05; 38% inhibition 13
Nitrofurantoin 1 mM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used β-hydroxybutyrate as substrate decrease Positive p < 0.05 13
Nitrofurantoin 50 μM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used β-hydroxybutyrate as substrate decrease Positive p < 0.05; 60% inhibition 13
Nitrofurantoin 5 μM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used β-hydroxybutyrate as substrate decrease Positive p < 0.05 13
Nitrofurantoin 1 mM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used α-ketoghttarate as substrate decrease Positive p < 0.05 13
Nitrofurantoin 50 μM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used α-ketoghttarate as substrate decrease Positive p < 0.05; 70% inhibition 13
Nitrofurantoin 5 μM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake; used α-ketoghttarate as substrate decrease Positive p < 0.05 13
nitrofurazone 1mM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.05; 64% inhibition 13
nitrofurazone 1mM mouse; C57B/6J liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.05; 63% inhibition 13
Perhexiline 200 μM 5 minutes preincubation mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 193
Perhexiline 400 μM 5 minutes preincubation mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake decrease Positive p < 0.01 193
nitrofurazone 5μM mouse; C57B/6J mitoplasts Measurement of oxygen uptake decrease Positive p < 0.05 13
nitrofurazone 5μM mouse; C57B/6J mitoplasts Measurement of oxygen uptake decrease Positive p < 0.05 13
Diazepam 70 μg/ml pig kidney embryo cells polarographic cell (1.2 ml) inhibit Positive 293
buformin 100 nmol/mg mitochondrial protein rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Phenformin 100 nmol/mg mitochondrial protein rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Metformin 500 nmol/mg mitochondrial protein 40 minutes preincubation rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
buformin 100 nmol/mg mitochondrial protein 40 minutes preincubation rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Phenformin 100 nmol/mg mitochondrial protein 40 minutes preincubation rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
buformin 100 nmol/mg mitochondrial protein rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Phenformin 100 nmol/mg mitochondrial protein rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Metformin 500 nmol/mg mitochondrial protein 40 min preincubation rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
buformin 100 nmol/mg mitochondrial protein 40 min preincubation rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Phenformin 100 nmol/mg mitochondrial protein 40 min preincubation rat; Sprague–Dawley liver mitochondria Meassurement of respiration decrease Positive 15
Perhexiline 100 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake increase Positive p < 0.01 193
Ketoconazole I50=32, 74, 65, 75, 500μM for substrates Glutamate/Malate, Pyruvate/Malate, Ornithine/Malate, Arginine/Malate and Succinate repectively rat liver mitochondria Clark electrode inhibit Positive 303
Perhexiline 100 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake increase Positive p < 0.01 193
Perhexiline 200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of oxygen uptake increase Positive p < 0.01 193