F0104 | Permeabilization
Transmembrane potential >> permeabilization
| Compound | Dose | Time | Species | Model | Method | Action | Result | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|---|
| Troglitazone | 10–75 μM | male CD-1 mice | isolated liver mitochondria | Mitochondrial swelling as the indicator of mitochondrial permeability transition (MPT) was estimated from the decrease in absorbance at 540 nm. | induce | Positive | 331 | ||
| Ciglitazone | 10–75 μM | male CD-1 mice | isolated liver mitochondria | Mitochondrial swelling as the indicator of mitochondrial permeability transition (MPT) was estimated from the decrease in absorbance at 540 nm. | induce | Positive | 331 | ||
| Cyclosporin A | inhibit | Positive | 248 | ||||||
| Troglitazone | 10 µM | 6hr | ZDF fa/fa rat vs ZDF lean rat | hepatocytes | Co2+-calcein assays; MPT pore opening was determined by measuring intensity of calcein fluorescence in the mitochondria quenched by cobalt and normalizing cell number of hoechst33342. | induce | Positive | significantly different from ZDF lean rats (p < 0.05) | 225 |
| Sulindac | increase | Positive | 45 | ||||||
| Troglitazone | increase | Positive | 7 | ||||||
| Cisplatin | U2OS | release of Smac m cherry(IMS-RP probe is a non-functional variant of mitochondrial protein Smac - mCherry fusion protein that acts as an indicator of mitochondrial permeabilization in live cells) | induce | Positive | 313 | ||||
| Thioridazine | increase | Positive | 49 | ||||||
| JW47 | 10nM | rat | liver mitochondria | Assess Ca2+-mediated PT pore formation by Calcium Retention Capacity Assay (Fluo-5N fluorescence was measured in the extramitochondrial solution following repeated additions of Ca2+) | inhibit | Positive | half-maximal inhibition | 324 | |
| Cyclosporin A | 40nM | rat | liver mitochondria | Assess Ca2+-mediated PT pore formation by Calcium Retention Capacity Assay (Fluo-5N fluorescence was measured in the extramitochondrial solution following repeated additions of Ca2+) | inhibit | Positive | half-maximal inhibition | 324 | |
| Chlorpromazine | >100 µM | 1 hour | Human | HepG2 | High-content screening assay | Affect | Positive | MEC | 306 |
| Nimesulide | Positive | 197 | |||||||
| Berberine | 31.2 nmol/mg | isolated rat muscle mitochondria | evaluate mitochondrial calcium loading capacity using the fluorescence probe Calcium Green 5N | induce | Positive | 327 | |||
| Cinnamic anilides | swellilng assay, Rhodamine 123 (Rh123) uptake assay, Calcium retention capacity assay | induce | Positive | 290 | |||||
| chenodeoxycholic acid | rat | isolated liver mitochondria | increase | Positive | 55 | ||||
| Bupivacaine | decrease | Positive | 61 | ||||||
| Amiodarone | 10 µM | 1 hour | Human | HepG2 | High-content screening assay | Increase | Positive | MEC | 306 |
| imipramine | 50 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| aristolochic acid | isolated kidney mitochondria | increase | Positive | 64 | |||||
| Maprotiline | 5 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| Rotenone | 5 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| Tamoxifen | 100 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| Troglitazone | 5 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| atorvastatin | 50 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| Diclofenac | 12.5 μmol/L | 10 minutes | rat | liver mitochondria | Assessment of MPT | increase | Positive | not mentioned | 6 |
| Diclofenac | 25 μmol/L | 10 minutes | rat | liver mitochondria | Assessment of MPT | increase | Positive | not mentioned | 6 |
| Diclofenac | 50 μmol/L | 10 minutes | rat | liver mitochondria | Assessment of MPT | increase | Positive | not mentioned | 6 |
| Diclofenac | 100 μmol/L | 10 minutes | rat | liver mitochondria | Assessment of MPT | increase | Positive | not mentioned | 6 |
| Menadione | increase | Positive | 35 | ||||||
| Troglitazone | 10 µM | 6hr | type 2 diabetes mellitus model rat | primary hepatocytes or isolated mitochondria | The loss of mitochondrial calcein and Hoechst 33342 nuclear fluorescence using a fluorescence microscope as an indicator of MPT for rat primary hepatocyte . Mitochondrial swelling as an indicator of MPT for isolated mitochondria. | Positive | 225 | ||
| Simvastatin | 10 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| Cerivastatin | 10 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| fluvastatin | 10 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| lovastatin | 50 µM | 1 hour | Human | HepG2 | High-content screening assay | Decrease | Positive | MEC | 306 |
| Troglitazone | increase | Positive | 35 | ||||||