Aminoglutethimide (BA-16038), an aromatase inhibitor, is used in the therapy of advanced BREAST Y.

Aromatase:10 μM

Aminoglutethimide在1至2周的服用后，将其自身的代谢速率从基础值的2.6±0.3 (S.E.) liters/24小时提高到5.3±1.4 liters/24小时，并显著加快人工合成的糖皮质激素dexamethasone的代谢速率，从基础值的145±26.6 liters/24小时提升至568±127 liters/24小时（p < 0.02）。[3] Aminoglutethimide（150 mg/kg）能够在成年雌性小鼠的卵巢和未成熟雄性小鼠的睾丸中，抑制由人绒毛膜促性腺激素(hCG)诱导的鸟氨酸脱羧酶(ODC)的表达，并几乎耗尽了由hCG引起的生殖腺和血浆中的孕酮或睾酮，这与对cAMP依赖性蛋白激酶的抑制（IC50 287 μM）有关，而非阻断类固醇生成途径。[4]

Concentration–response and kinetic studies: The microsomal protein (30 μg), [1β-3H]androstenedione (6.6 × 105 dpm) and NADPH (270 μM) are used for the concentration–response experiment with an incubation time of 20 minutes. The Aminoglutethimide is initially tested at 10 μM and 100 μM concentrations, followed by a full concentration–response study with at least 8 concentrations ranging from 0.01 μM to 160 μM. For the initial velocity study the concentration of [1β-3H]androstenedione is varied from 7.5 to 100 nM and the incubation time is set to 5 minutes. The tritiated water formed during the conversion of the tritiated substrate, [1β-3H]androstenedione, to estrone is quantified by liquid scintillation counting. Each assay is performed three times in duplicate and the results are treated by nonlinear regression analysis allowing the determination of the half-maximal inhibitory concentration (IC50).

The NCI-h295 tumor cell line is maintained in RPMI 1640 medium supplemented with transferrin (0.1 mg/mL), insulin (5 μg/mL), selenium (5.2 μg/mL) and 2% FCS. The cells are incubated for 48 hours with Aminoglutethimide (3, 30, 300 μM). Then cells are examined by trypan blue staining for cell viability, counted 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.(Only for Reference)