货号:A829627 同义名: 盐酸哌唑嗪 / Prazosin (hydrochloride);cp-12299-1
Prazosin HCl is a selective α-1-adrenergic receptor antagonist used to treat hypertension, anxiety, and posttraumatic stress disorder (PTSD).
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产品名称 | Adrenergic Receptor ↓ ↑ | α-adrenergic receptor ↓ ↑ | β-adrenergic receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ivabradine HCl | ✔ | 98% | |||||||||||||||||
Maprotiline hydrochloride | ✔ | 98% | |||||||||||||||||
Cisatracurium besylate | ✔ | 98% | |||||||||||||||||
Yohimbine HCI | ✔ | 99+% | |||||||||||||||||
BMY 7378 |
++
α2C-adrenoceptor, pKi: 6.54 α1D-adrenoceptor, pKi: 5.1 |
+
β1-adrenoceptor, pIC50: 5.1 |
97% | ||||||||||||||||
Asenapine maleate |
++++
α2A-adrenergic receptor, pKi: 8.9 α2B-adrenergic receptor, pKi: 8.9 |
97% | |||||||||||||||||
Piribedil |
++
adrenoceptor α2C, pKi: 7.2 adrenoceptor α2A, pKi: 7.1 |
98% | |||||||||||||||||
Prazosin HCl | ✔ | 95% | |||||||||||||||||
Silodosin | ✔ | 98% | |||||||||||||||||
Phenoxybenzamine HCl | ✔ | 98% | |||||||||||||||||
Naftopidil |
+++
α1A-adrenergic receptor, Ki: 3.7 nM α1D-adrenergic receptor, Ki: 20 nM |
98% | |||||||||||||||||
Naftopidil 2HCl |
+
α1-adrenergic receptor, IC50: 0.2 μM |
97% | |||||||||||||||||
Alfuzosin HCl | ✔ | 98% | |||||||||||||||||
Terazosin HCl | ✔ | 99% | |||||||||||||||||
Atipamezole | ✔ | 95% | |||||||||||||||||
Phentolamine methanesulfonate salt | ✔ | 99% | |||||||||||||||||
Doxazosin mesylate | ✔ | 98% | |||||||||||||||||
Tolazoline HCl | ✔ | 98% | |||||||||||||||||
Zenidolol hydrochloride |
++++
β1-adrenergic receptor, Ki: 611nM β2-adrenergic receptor, Ki: 0.7nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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]. |
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 << |
[3]Green B. Prazosin in the treatment of PTSD. J Psychiatr Pract. 2014;20(4):253-259
[5]Jaillon P. Clinical pharmacokinetics of prazosin. Clin Pharmacokinet. 1980;5(4):365-376
计算器 | ||||
存储液制备 | 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 |
CAS号 | 19237-84-4 |
分子式 | C19H22ClN5O4 |
分子量 | 419.862 |
别名 | 盐酸哌唑嗪 ;Prazosin (hydrochloride);cp-12299-1;NSC 292810;Prazosin hydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
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 |