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Monocrotaline (Crotaline) is an pyrrolizidine alkaloid extracted from the seeds of the Crotalaria spectabilis plant to induce pulmonary hypertension in rodents. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | Brain endothelial cells |
| Preparation method | Cell viability was analyzed through the activity of mitochondrial dehydrogenases by the tetrazolium salts reduction test, which is performed by a sensitive, quantitative, and reliable colorimetric measurement, used to measure cell viability, proliferation, and metabolic activity. Its principle is based on the ability of living cell mitochondrial dehydrogenases to convert 3-(-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT), a yellow substrate, from formazan crystals to a violet-colored substrate. For this, BECs were cultivated in polystyrene plates (TPP) containing 96 wells (3.1 × 10^4 cells/cm2) over a collagen layer and after 24 and 72 h submitted to treatment with MCT at concentrations of 1, 10, 100, and 500 µM. |
| Concentrations | 1, 10, 100, and 500 µM |
| Incubation time | 24 and 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague–Dawley rats |
| Formulation | MCT was completely dissolved in 1 N HCl, the pH was adjusted to 7.4 with 0.5 N NaOH, and the solution was then diluted with sterile PBS. |
| Dosages | 60 mg/kg |
| Administration | Subcutaneous injection |
| Molecular Weight | 325.36 |
| Formula | C16H23NO6 |
| CAS Number | 315-22-0 |
| Solubility (25°C) | 1M HCl: 90 mg/mL (adjust pH to 1 with HCl) DMSO 25 mg/mL |
| Storage | 4°C, protect from light, dry, sealed |
[6] Amy L Firth, et al. Idiopathic pulmonary arterial hypertension
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