Aminoglutethimide (Cytadren) is an inhibitor of adrenocortical steroid synthesis. It blocks aromatase in the generation of estrogens from androstenedione and testosterone. It also blocks the conversion of cholesterol to pregnenolone by inhibiting the enzyme P450scc and consequently decreases synthesis of all hormonally active steroids. It inhibited bovine adrenal cholesterol side-chain cleavage activity with an IC50 value of 40 μM.
| Cell Experiment | |
|---|---|
| Cell lines | Adrenocortical tumor cell line NCI-h295 |
| Preparation method | Maintaining the NCI-h295 tumor cell line in RPMI 1640 medium which is supplemented with transferrin (0.1 mg/mL), insulin (5 μg/mL), selenium (5.2 μg/mL) and 2% FCS. Incubating the cells for 48 hours with Aminoglutethimide (3, 30, 300 μM). Then examining cells by trypan blue staining for cell viability, counting with a coulter counter. For the assessment of ACTH-R mRNA, cells are harvested, and total RNA is extracted, electrophoresed, blotted and hybridized with a human ACTH-R cDNA probe. |
| Concentrations | Dissolved in 65% ethanol as a stock solution, final concentrations 3, 30, 300 μM. |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Swiss CD1 male and female mice |
| Formulation | Dissolved in DMSO and diluted in saline. |
| Dosages | 150 mg/kg |
| Administration | Injection |
| Molecular Weight | 232.28 |
| Formula | C13H16N2O2 |
| CAS Number | 125-84-8 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] G Cocconi. First generation aromatase inhibitors--aminoglutethimide and testololactone
[2] R J Santen, et al. Aminoglutethimide: review of pharmacology and clinical use
[3] No authors listed. Lancet. Aminoglutethimide
[4] S W Hughss, et al. Aminoglutethimide: a "side-effect" turned to therapeutic advantage
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