Terazosin hydrochloride dihydrate 是一种竞争性和口服活性的 α1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,是一种喹唑啉衍生物,通过舒张血管和打开膀胱的方式起作用。它可用于研究良性前列腺增生 (BPH) 和高血压。
产品描述
Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
体外活性
Terazosin results in a significant loss of cell viability, via induction of apoptosis in a dose-dependent manner in prostate cancer cells. Terazosin suppresses prostate growth potentially via α 1-adrenoceptor-independent actions gains further support from another study documenting that Doxazosin inhibits proliferation of human vascular smooth muscle cells independently of an antagonistic effect on α1-adrenoceptor. [1] Terazosin blocks HERG currents in Xenopus oocytes with IC50 of 113.2 mM, while Terazosin blocks HERG channel inhibition in human HEK 293 cells with IC50 of 17.7 mM. [2] Terazosin or genistein treatment inhibits the growth of DU-145 cells in a dose-dependent manner, whereas has no effect on normal prostate epithelial cells. Terazosin results in the genistein-induced arrest of DU-145 cells in G2/M phase being overridden and an increase in apoptotic cells, as evidenced by procaspase-3 activation and PARP cleavage. [3] Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 mM. [4]
体内活性
Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 mM, showing that it has a more potent anti-angiogenic than cytotoxic effect. Terazosin also effectively inhibits vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 mM, respectively). [4]
Cas No.
70024-40-7
分子式
C19H30ClN5O6
分子量
459.93
别名
Flotrin dihydrate;Dysalfa dihydrate;盐酸特拉唑嗪(二水合物);Terazosin HCl Dihydrate;Heitrin dihydrate
储存和溶解度
DMSO:25 mg/mL (54.4 mM)
Ethanol:<1 mgml
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years