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Prazosin HCl

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Chemical Structure| 19237-84-4 同义名 : 盐酸哌唑嗪 ;Prazosin (hydrochloride);cp-12299-1;NSC 292810;Prazosin hydrochloride
CAS号 : 19237-84-4
货号 : A829627
分子式 : C19H22ClN5O4
纯度 : 95%
分子量 : 419.862
MDL号 : MFCD00058177
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(35.73 mM)，配合低频超声助溶，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 Prazosin Hydrochloride, an a1-adrenoceptor blocker, has shown some promise in treating chronic PTSD (Posttraumatic stress disorder). Treatment of PTSD with prazosin is usually initiated at a dose of 1 mg, with monitoring for hypotension after the first dose. The dose is then gradually increased to maintenance levels of 2-6 mg at night[3]. Prazosin has been shown to be effective in the treatment of PTSD trauma-related nightmares, with low side effect profile and abilities to improve both sleep and reduce trauma nightmares[4]. Prazosin is extensively metabolised by the liver and has high first-pass metabolism and low oral bioavailability. Oral bioavailability of prazosin ranges from 43.5 to 69.3% (mean 56.9%). Prazosin is highly (92 to 97%) bound to human plasma proteins (albumin and alpha 1-acid glycoprotein) and the extent of binding is independent of the plasma concentration of the drug in the range of 20 to 150 ng/mL[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
NCT01677767 - Completed - India ... 展开 >> Sir Gangaram Hospital New Delhi, Delhi, India, 110060 Ahmedabad Dialysis Centre Ahmedabad, India, 380005 Excel Center Guwahati, India, 781007 ESIS Hospital; Department of Nephrology Kolkata, India, 600054 Vertex Hospital Mumbai, India, 400083 Apollo Indraprastha Hospitals; Nephrology New Delhi, India, 110076 Aditya Birla Memorial Hospital Pune, India, 411033 收起 <<
NCT00687388 Benign Prostatic Hyperplasia Phase 4 Withdrawn(in order to prepare ... 展开 >>a new clinical trial to evaluate with pathological change) 收起 << - Korea, Republic of ... 展开 >> Severance Hospital Seoul, Korea, Republic of, 120-752 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Asan Medical Center Seoul, Korea, Republic of, 138-736 收起 <<
NCT01030874 Orthostatic Hypotension ... 展开 >> Falls 收起 << Not Applicable Completed - United States, Oregon ... 展开 >> VA Portland Health Care System, Portland, OR Portland, Oregon, United States, 97239 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.91mL

2.38mL

1.19mL

23.82mL

4.76mL

2.38mL
参考文献

[1]Baum O, Da Silva-Azevedo L, et al. Endothelial NOS is main mediator for shear stress-dependent angiogenesis in skeletal muscle after prazosin administration. Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2300-8.

[2]Yu CX, Zhu CB, et al. Selective MT(2) melatonin receptor antagonist blocks melatonin-induced antinociception in rats. Neurosci Lett. 2000 Mar 24;282(3):161-4.

[3]Green B. Prazosin in the treatment of PTSD. J Psychiatr Pract. 2014;20(4):253-259

[4]Breen A, Blankley K, Fine J. The efficacy of prazosin for the treatment of posttraumatic stress disorder nightmares in U.S. military veterans. J Am Assoc Nurse Pract. 2017;29(2):65-69

[5]Jaillon P. Clinical pharmacokinetics of prazosin. Clin Pharmacokinet. 1980;5(4):365-376