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 |