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Terazosin HCl

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Chemical Structure| 63074-08-8 同义名 : Terazosin (hydrochloride);Hytrin;A-45975;Hyprin;Vasocard;Terazocin HCl;Blavin;Fosfomic;Flumarc;Terazosine;Zayasel;Terazosin hydrochloride
CAS号 : 63074-08-8
货号 : A283609
分子式 : C19H26ClN5O4
纯度 : 99%
分子量 : 423.894
MDL号 : MFCD00467965
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(37.75 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • α-adrenergic receptor
描述 Terazosin hydrochloride is one of long-acting α-blockers and commonly used agent for treating BPH(benign prostatic hyperplasia) and/or hypertension. LD50s of terazosin were 277 and 293 mg kg−1 for male and female rats, respectively, after i.v. administration of the drug[3]. Use of oral terazosin hydrochloride (1.5 mg, orally or subcutaneously) elevated flap survival rates to control levels in nicotine-treated rats[4]. Moreover, terazosin reduces tumor vascularity and induces apoptosis in TCC(transitional cell carcinoma) of the bladder[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00000620 Atherosclerosis ... 展开 >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease 收起 << Phase 3 Completed - United States, Minnesota ... 展开 >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada 收起 <<
NCT03339258 Stress Disorders, Post-Traumat... 展开 >>ic 收起 << Phase 2 Recruiting June 2021 United States, California ... 展开 >> San Francisco VA Medical Center Recruiting San Francisco, California, United States, 94121 Contact: Andrew Levihn-Coon, B.A.    415-221-4810 ext 23809    andrew.levihn-coon@va.gov 收起 <<
NCT01323998 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL
参考文献

[1]Pan SL, Guh JH, et al. Identification of apoptotic and antiangiogenic activities of terazosin in human prostate cancer and endothelial cells. J Urol. 2003 Feb;169(2):724-9.

[2]Stone EA, Zhang Y, et al. Brain alpha 1-adrenergic neurotransmission is necessary for behavioral activation to environmental change in mice. Neuroscience. 1999;94(4):1245-52.

[3]Oh EY, Bae SK, Kwon JW, You M, Lee DC, Lee MG. Pharmacokinetic and pharmacodynamic consequences of inhibition of terazosin metabolism via CYP3A1 and/or 3A2 by DA-8159, an erectogenic, in rats. Br J Pharmacol. 2007 May;151(1):24-34. doi: 10.1038/sj.bjp.0707192. Epub 2007 Mar 12. PMID: 17351661; PMCID: PMC2012980.

[4]Karien RG, Maisel RH. Terazosin blockade of nicotine-induced skin flap necrosis in the rat. Arch Otolaryngol Head Neck Surg. 1997 Aug;123(8):837-40. doi: 10.1001/archotol.1997.01900080069008. PMID: 9260549.

[5]Tahmatzopoulos A, Lagrange CA, Zeng L, Mitchell BL, Conner WT, Kyprianou N. Effect of terazosin on tissue vascularity and apoptosis in transitional cell carcinoma of bladder. Urology. 2005 May;65(5):1019-23. doi: 10.1016/j.urology.2004.12.015. PMID: 15882756; PMCID: PMC2274913.