Doxazosin mesylate能选择性拮抗突触后的α1肾上腺素受体。
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.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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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