Doxazosin mesylate 是一种喹唑啉衍生物。它是一种选择性拮抗突触后α1-肾上腺素能受体。

Doxazosin mesylate(UK 33274) is a quinazoline-derivative. It is a selectively antagonizes postsynaptic α1-adrenergic receptors.

Doxazosin降低平均动脉压为18％,但不会影响所有仓鼠的心脏速率.Doxazosin显著降低Beta TGF-β1感染小鼠前列腺重建（MPR）的湿重.

Doxazosin和消胆胺类似地降低血浆总胆固醇,LDL加VLDL胆固醇和平均总甘油三酯分别达46％,61％和45％。Doxazosin减少乳鼠心肌细胞原代培养细胞的活力,Hoechst染色活体染色表明Doxazosin诱导人成心肌细胞的凋亡。Doxazosin 在HL-1细胞系中,诱导DNA损伤和细胞死亡。Doxazosin诱导细胞凋亡是由特定的胱天蛋白酶-8抑制剂阻断,caspase-8功能性参与Doxazosi诱导的细胞凋亡。 Doxazosin拮抗HUVEC细胞的VEGF介导的血管生成响应,通过废除细胞粘附到纤连蛋白和胶原包被的表面,并抑制细胞迁移,通过血管内皮生长因子的表达的下调。Doxazosin增加FADD招募和caspase-8激活,暗示Fas介导细胞凋亡,作为Doxazosin在前列腺细胞中作用的基本机制。

Protease assays: To determine the inhibition constants (Ki) for each Prt inhibitor, purified HIV-1 RF wild-type Prt (2.5 nM) is incubated at 37 ℃ with 1 μM to 15 μM fluorogenic substrate in reaction buffer (1 M NaCl, 1 mM EDTA, 0.1 M sodium acetate [pH 5.5], 0.1% polyethylene glycol 8000) in the presence or absence of Atazanavir. Cleavage of the substrate is quantified by measuring an increase in fluorescent emission at 490 nM after excitation at 340 nM using a Cytofluor 4000. Reactions are carried out using 1.36 μM, 1.66 μM, 2.1 μM, 3.0 μM, 5.0 μM, or 15 μM substrate in the presence of five concentrations of Atazanavir (1.25 nM to 25 nM). Substrate cleavage is monitored at 5-min intervals for 30 min. Cleavage rates are then determined for each sample at early time points in the reaction, and Ki values are determined from the slopes of the resulting Michaelis-Menten plots.

77883-43-3

C24H29N5O8S

547.58

甲磺酸多沙唑嗪;UK 33274 mesylate

DMSO:41.1 mg/mL (75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years