Doxazosin Mesylate

甲磺酸多沙唑嗪,UK 33274 mesylate

Doxazosin mesylate能选择性拮抗突触后的α1肾上腺素受体。

目录号
EY0693
EY0693
纯度
99.37%
99.37%
规格
100 mg
500 mg
原价
450
1400
售价
450
1400
库存
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Doxazosin Mesylate is an α-blocker drug related to prazosin, specifically acting as an AR (α-1-adrenoceptor) antagonist. Selective α1-adrenoceptor antagonist (pKi values are 9.0, 8.5 and 8.4 for human α1B, α1A and α1D receptors respectively). Displays antihypertensive activity. Doxazosin Mesylate inhibits the binding of norepinephrine to the α-1 receptors on the membrane of vascular smooth muscle cells. The primary effect of this inhibition is relaxed vascular smooth muscle tone (vasodilation), which decreases peripheral vascular resistance, leading to decreased blood pressure.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Garrison JB, et al. Cancer Res, 2006, 66(1), 464-472.
    [2] McConnell, J.D., et al. 2003. N. Engl. J. Med. 349: 2387-2398.
    [3] Stafford, R.S., et al. 2004. JAMA. 291: 54-62.

    分子式
    C24H29N5O8S
    分子量
    547.58
    CAS号
    77883-43-3
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    15 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01003886 Prostatic Hyperplasia Drug: Doxazosin mesylate GITS Pfizer 2009-05-01 2011-09-19
    NCT01062945 Cocaine Addiction|Cocaine Abuse|Cocaine Dependence|Substance Abuse Drug: Placebo|Drug: Doxazosin Baylor College of Medicine|National Institute on Drug Abuse (NIDA) Phase 1 2010-01-01 2012-07-25
    NCT01959022 Stress Disorders, Post-Traumatic Drug: Doxazosin XL San Francisco Veterans Affairs Medical Center|United States Department of Defense|Northern California Institute of Research and Education Phase 4 2013-10-01 2016-10-19
    NCT01145183 Cocaine Dependence Drug: Doxazosin|Drug: Placebo Baylor College of Medicine|National Institute on Drug Abuse (NIDA) Phase 2 2010-03-01 2017-02-04
    NCT02492334 PTSD|Alcohol Use Disorder Drug: Doxazosin|Drug: Placebo Medical University of South Carolina|Ralph H. Johnson VA Medical Center Phase 1|Phase 2 2016-07-01 2016-05-11
    NCT00880997 Cocaine Dependence Drug: Doxazosin|Drug: Placebo Baylor College of Medicine|National Institute on Drug Abuse (NIDA) Phase 1 2009-09-01 2012-10-22
    NCT01730846 Smoking Drug: Doxazosin|Drug: Placebo Yale University|National Institute on Drug Abuse (NIDA) Phase 2 2013-02-01 2016-11-22
    NCT02500602 Posttraumatic Stress Disorder|Alcohol Use Disorders Drug: doxazosin xL|Drug: placebo VA Office of Research and Development|Medical University of South Carolina|Consortium to Alleviate PTSD Phase 2 2016-06-01 2017-01-06
    NCT00922506 Overactive Bladder|Benign Prostatic Hyperplasia Drug: doxazosin plus tolterodine SR Samsung Medical Center Phase 4 2009-05-01 2015-02-12
    NCT00730418 Benign Prostatic Hyperplasia Drug: Doxazosin|Drug: Doxazosin Samsung Medical Center 2007-01-01 2010-08-25
    NCT01386177 Mood Disorder|Substance-Related Disorders|Amphetamine-Related Disorders Drug: 3,4-Methylenedioxymethamphetamine|Drug: Doxazosin|Drug: placebo University Hospital, Basel, Switzerland Phase 1 2011-07-01 2016-01-20
    NCT01371851 Methamphetamine or Cocaine Dependence Drug: Doxazosin extended release University of Arkansas|National Institute on Drug Abuse (NIDA)|Baylor College of Medicine Phase 1|Phase 2 2011-06-01 2015-07-24
    NCT01437046 Alcohol Dependence|Anxiety Drug: Doxazosin|Drug: Placebo Brown University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Phase 2 2011-11-01 2015-07-20
    NCT02989493 Alcoholism Drug: Doxazosin|Other: Placebo University of Wisconsin, Madison|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Phase 2 2017-01-01 2016-12-07
    NCT01379898 Pheochromocytoma Drug: Phenoxybenzamine|Drug: Doxazosin University Medical Center Groningen|Radboud University|UMC Utrecht|VU University of Amsterdam|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Leiden University Medical Center|Erasmus Medical Center|Maastricht University Medical Center|St. Antonius Hospital|Medisch Spectrum Twente|Maxima Medical Center|Canisius-Wilhelmina Hospital|Onze Lieve Vrouwe Gasthuis|Atrium Medical Center|Isala Phase 4 2011-12-01 2016-10-25
    NCT00646841 Hypertension Drug: Doxazosin gastrointestinal therapeutic system (GITS) Pfizer Phase 4 2003-02-01 2008-08-07
    NCT01389609 Hypertension Drug: Doxazosin 4 mg Japanese marketed IR tablet|Drug: Doxazosin 4 mg ODT with water|Drug: Doxazosin 4 mg ODT without water Pfizer Phase 1 2011-07-01 2011-10-05
    NCT01953432 Cocaine Dependence Drug: Doxazosin|Drug: Placebo VA Office of Research and Development|Baylor College of Medicine Phase 2 2014-04-01 2016-09-13
    NCT02308202 PTSD Drug: doxazosin|Drug: Perindopril|Drug: Placebo Baylor College of Medicine Phase 1 2012-01-01 2016-09-27
    NCT02901977 Hypertension Drug: Ramipril|Drug: Doxazosin Karolinska Institutet Phase 4 2011-03-01 2016-09-10
    NCT01100021 Erectile Dysfunction Drug: Tamsulosin and avanafil|Drug: Doxazosin and avanafil VIVUS, Inc. Phase 1 2010-02-01 2011-01-05
    NCT02563405 Hypertension Drug: Doxazosin|Drug: Nifedipine First Affiliated Hospital of Harbin Medical University Phase 2|Phase 3 2015-09-01 2016-07-26

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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