Anastrozole (ZD1033)(ZD1033), a potent and highly selective aromatase (CYP19) inhibitor (IC50 = 15 nM), has no obvious effect on adrenocorticoid hormone synthesis.

Aromatase:15 nM

以Anastrozole（>9.1 mg/kg）对雄性尾纤猴每天两次给药,其外周芳香化酶会被抑制,使得循环雌二醇的浓度减少到50%~60%.给成熟大鼠每2~3个发情周期口服0.1 mg/kg Anastrozole,可阻断成熟雌性大鼠的排卵;以某些剂量对青春期大鼠给药3天,可完全阻断雄烯二酮刺激的子宫发育.这些作用也许是因为抑制了成熟雌性动物正常排卵期前体内卵泡中雌激素合成的升高,而在青春期雌性动物体内,则抑制了其不成熟卵巢代谢外源性雄烯二酮.

Anastrozole能够结合芳香化酶CYP单元中的血红素基团从而竞争性地抑制该酶,减少乳腺和外周中雌激素的生物合成。Anastrozole对其它甾体激素几乎没有作用。在体外Anastrozole具有较高固有效力,可抑制人胎盘的芳香化酶（IC50：15 nM）。Anastrozole的效果是4-OHA的2倍,AG的200倍,法倔唑的三分之一。

Aromatase inhibition is measured using human placental microsomes and the method of Thompson and Siiteri with Testosterone (0.5 μM) as substrate. 11-hydroxylase inhibition is determined by measuring the conversion of [1,2,6,7-3H]-ll-deoxy- cortisol to cortisol using freshly prepared mitochondria from guinea pig, dog and cow adrenal glands. Reaction products are extracted into chloroform and separated by thin layer chromatography[1].