| Tamoxifen |
|
|
|
|
|
affect |
Positive |
|
227 |
| Perhexiline |
100 μM |
5 minutes preincubation; 10 minutes |
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of beta oxidation |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
100 μM |
5 minutes preincubation; 10 minutes |
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of beta oxidation |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
200 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
400 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
800 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
1200 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
200 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
400 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
800 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
1200 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
1600 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
400 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.05 |
193 |
| Perhexiline |
800 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
1200 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
1600 μM |
|
mouse; Crl/CD-l(1CR)BR Swiss |
liver mitochondria |
Measurement of activities of acyl-CoA dehydrogenases |
decrease |
Positive |
p < 0.01 |
193 |
| Perhexiline |
|
|
|
|
|
decrease |
Positive |
|
16 |
| Perhexiline |
|
|
|
|
|
decrease |
Positive |
|
16 |
| buprenorphine |
100 μM |
|
rat |
liver mitochondria |
the mitochondrial membrane potential assessed by the fluorescence of safranine. |
affect |
Positive |
|
235 |
| Tianeptine |
0.0625 mmol/kg i.p. |
|
mouse |
|
in vivo |
affect |
Positive |
|
237 |
| Perhexiline |
|
|
|
|
|
decrease |
Positive |
|
17 |
| Perhexiline |
|
|
|
|
|
decrease |
Positive |
|
17 |
| Trimetazidine |
|
|
|
|
|
decrease |
Positive |
|
17 |
| ranolazine |
|
|
|
|
|
decrease |
Positive |
|
17 |
| tetracyclines |
|
|
mouse |
liver mitochondria |
|
affect |
Positive |
|
236 |
| 5-Hydroxydecanoate |
100 μm |
|
|
|
|
decrease |
Positive |
|
189 |
| 5-Hydroxydecanoate |
K1/2 values 45-75 microM |
|
|
heart and liver mitochondria from rat |
|
decrease |
Positive |
|
190 |
| Ibuprofen |
|
|
|
|
|
affect |
Positive |
|
239 |
| Perhexiline |
77 μmol/L |
|
rat |
cardiac mitochondria |
CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, |
affect |
Positive |
IC50 |
240 |
| Perhexiline |
148 μmol/L |
|
rat |
hepatic mitochondria |
CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, |
affect |
Positive |
IC50 |
240 |
| Amiodarone |
228 μmol/L |
|
rat |
cardiac and hepatic mitochondria |
CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, |
affect |
Positive |
IC50 |
240 |
| FOX-988 |
|
|
|
|
|
decrease |
Positive |
|
28 |
| Acetaminophen |
>400μM |
>400 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Sdz-51641 |
|
|
|
|
|
decrease |
Positive |
|
28 |
| Salicylic acid |
|
|
|
|
|
decrease |
Positive |
|
32 |
| Irinotecan |
6μM |
10 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Methotrexate |
44μM |
42 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Troglitazone |
|
|
|
|
|
affect |
Positive |
|
227 |
| Valproic Acid |
|
|
|
|
|
affect |
Positive |
|
227 |
| Perhexiline |
|
|
|
|
|
decrease |
Positive |
|
35 |
| Amiodarone |
20 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| Amiodarone |
50 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| Amiodarone |
80 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| Amiodarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| benzarone |
20 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| benzarone |
50 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| benzarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| benzbromarone |
2 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.05 |
4 |
| benzbromarone |
5 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| benzbromarone |
10 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| benzbromarone |
50 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| 2‐Butylbenzofuran |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of beta oxidation and ketone body formation |
decrease |
Positive |
p < 0.01 |
4 |
| Etomoxir |
|
|
|
|
|
decrease |
Positive |
|
35 |
| Salicylic acid |
|
|
|
|
|
decrease |
Positive |
|
35 |
| Carbamazepine |
>400μM |
341 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Diclofenac |
47μM |
11* |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Ibuprofen |
287μM |
80* |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Amiodarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of acyl‐CoA dehydrogenase activity |
decrease |
Positive |
28% inhibition |
4 |
| benzarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of acyl‐CoA dehydrogenase activity |
decrease |
Positive |
33% inhibition |
4 |
| benzbromarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of acyl‐CoA dehydrogenase activity |
decrease |
Positive |
34% inhibition |
4 |
| 2‐Butylbenzofuran |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of acyl‐CoA dehydrogenase activity |
decrease |
Positive |
22% inhibition |
4 |
| benzarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of β‐ketothiolase activity |
decrease |
Positive |
11% inhibition |
4 |
| benzbromarone |
100 μmol/L |
|
rat; Sprague–Dawley |
liver mitochondria |
Measurement of β‐ketothiolase activity |
decrease |
Positive |
25% inhibition |
4 |
| Salicylic acid |
>400μM |
>400 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Tamoxifen |
4μM |
11 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Perhexiline |
|
|
rat |
hepatocytes |
|
affect |
Positive |
|
238 |
| Zidovudine |
79μM |
83 |
mice |
Lean mice vs Ob/ob mice |
Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform |
|
Positive |
EC20 |
227 |
| Acetaminophen |
|
|
|
|
|
affect |
Positive |
|
227 |
| amineptine |
|
|
|
|
|
decrease |
Positive |
|
54 |
| pirprofen |
|
|
|
|
|
decrease |
Positive |
|
59 |
| Salicylic acid |
|
|
|
|
|
affect |
Positive |
|
227 |
| Ibuprofen |
|
|
|
|
|
affect |
Positive |
|
227 |
| TDGA |
<0.05/0.04 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| POCA |
10.4/95.9 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Etomoxir |
0.29/0.34 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| DET |
1.8/4.4 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| aminocarnitine |
−/− |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Carnitine |
0.5mM |
24hr |
|
U-937, MCF-7, and T47D |
quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion |
stimulate |
Positive |
|
273 |
| AICAR |
1mM |
24hr |
|
U-937, MCF-7, and T47D |
quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion |
stimulate |
Positive |
|
273 |
| AICAR |
|
|
|
|
|
stimulate |
Positive |
|
273 |
| palmitoylaminocarnitine |
2.8/0.27 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| ST1326 |
4.0/0.98 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| ST2425 |
0.73/0.03 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Trimetazidine |
20.5/>100 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Perhexiline |
22.4/21.4 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Amiodarone |
28.5/>100 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Oxfenicine |
>100/>100 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| oxfenicine metabolite |
33.3/>100 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| RO-25-0187 |
25.5/>100 |
|
human/rat |
hepatocytes |
Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate |
inhibition |
Positive |
IC50 (μM) |
333 |
| Hypoglycin A |
|
|
|
|
|
|
Positive |
|
232 |
| 4-Pentenoic acid |
|
|
|
|
|
|
Positive |
|
232 |
| 2-bromooctanoic acid |
|
|
|
|
|
|
Positive |
|
232 |
| 2-tetradecylglycidic acid |
|
|
|
|
|
|
Positive |
|
232 |
| 2-bromopalmitic acid |
|
|
|
|
|
|
Positive |
|
232 |
| Palmitoylcarnitine |
|
|
|
|
|
|
Positive |
|
232 |
| Perhexiline |
5 μM |
72 hours |
rat; Sprague-Dawley Crl:CD-1 (ICR) BR |
hepatocytes |
Measurement of beta oxidation |
decrease |
Positive |
p < 0.05 |
193 |
| Perhexiline |
25 μM |
24 hours |
rat; Sprague-Dawley Crl:CD-1 (ICR) BR |
hepatocytes |
Measurement of beta oxidation |
decrease |
Positive |
p < 0.05 |
193 |
| Amiodarone |
|
|
|
|
|
affect |
Positive |
|
227 |
| Tamoxifen |
|
|
|
|
|
affect |
Positive |
|
227 |