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/ 肾上腺素能受体 / Prazosin HCl/哌唑嗪盐酸盐

Prazosin HCl/哌唑嗪盐酸盐 {[allProObj[0].p_purity_real_show]}

货号：A829627 同义名： 盐酸哌唑嗪 / Prazosin (hydrochloride); cp-12299-1

Prazosin HCl 是一种选择性 α1-肾上腺素受体拮抗剂，常用于高血压、焦虑及创伤后应激障碍（PTSD）相关神经调控机制研究。

Prazosin HCl/哌唑嗪盐酸盐 化学结构 CAS号：19237-84-4
Prazosin HCl/哌唑嗪盐酸盐 化学结构
CAS号：19237-84-4
Prazosin HCl/哌唑嗪盐酸盐 3D分子结构
CAS号：19237-84-4
Prazosin HCl/哌唑嗪盐酸盐 化学结构 CAS号：19237-84-4
Prazosin HCl/哌唑嗪盐酸盐 3D分子结构 CAS号：19237-84-4
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Prazosin HCl/哌唑嗪盐酸盐 纯度/质量文件 产品仅供科研

货号：A829627 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 HCl ✔ 98%
Cisatracurium besylate ✔ 96%
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 α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

 		98%
Prazosin HCl ✔ 95%
Silodosin ✔ 98%
Phenoxybenzamine HCl ✔ 98%
Labetalol HCl ✔ 98+%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		99%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Carvedilol ✔ 99%
Doxazosin mesylate ✔ 99%
Tolazoline HCl ✔ 98%
Esmolol HCl ✔ 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

 		99%
Zenidolol HCl ++++

β2-adrenergic receptor, Ki: 0.7nM

β1-adrenergic receptor, Ki: 611nM

 		98%
Acebutolol HCl ✔ 97+%
Carteolol HCl ✔ 98+%
Betaxolol ✔ 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

 		97%
Bisoprolol ✔ 97%
Sotalol HCl ✔ 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

 		99%
Metoprolol ✔ 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。

Prazosin HCl/哌唑嗪盐酸盐 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].

Prazosin HCl/哌唑嗪盐酸盐 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293T cells 10 μM 6–8 h Cell protection Nat Commun. 2023 Aug 10;14(1):4819.
HEK 293T cells 150 nM 2 h To measure the binding of Prazosin to the α1A adrenergic receptor, results showed that Prazosin could competitively bind to the receptor. J Biol Chem. 2021 Jan-Jun;296:100366.
HuH-7R cells 10 μM Prazosin inhibits Akt activity by targeting the ligand-binding domain of EphA2, reducing EphA2 Ser897 phosphorylation, thereby inhibiting cell migration and invasion. Exp Mol Med. 2020 Mar;52(3):497-513.
HuH-7R cells 10 μM 0, 2, 4, 6 h Prazosin induces EphA2 internalization, triggering apoptosis and inhibiting migration and invasion of HuH-7R cells. Exp Mol Med. 2020 Mar;52(3):497-513.
YD-8/CIS 250 nM 30 min To monitor BCRP activity, results showed reduced accumulation of prazosin in YD-8/CIS cells, indicating increased BCRP activity. Int J Mol Sci. 2019 Jun 21;20(12):3034.
YD-9/CIS 250 nM 30 min To monitor BCRP activity, results showed reduced accumulation of prazosin in YD-9/CIS cells, indicating increased BCRP activity. Int J Mol Sci. 2019 Jun 21;20(12):3034.
YD-38/CIS 250 nM 30 min To monitor BCRP activity, results showed reduced accumulation of prazosin in YD-38/CIS cells, indicating increased BCRP activity. Int J Mol Sci. 2019 Jun 21;20(12):3034.

Prazosin HCl/哌唑嗪盐酸盐 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Subcutaneous xenograft tumor model Oral 3 mg/kg Once daily for 18 days Prazosin alone or in combination with sorafenib significantly inhibits tumor growth and prolongs the survival of tumor-bearing mice. Exp Mol Med. 2020 Mar;52(3):497-513.
Mice PTP1B KO mice Intraperitoneal injection 2 mg/kg Once daily for 7 days To assess the effect of Prazosin on vascular adrenergic reactivity, results showed that Prazosin restored vascular adrenergic reactivity in PTP1B KO mice. Circulation. 2009 Sep 1;120(9):753-63
Mice IP3R2−/− mice Intraperitoneal injection 1 mg/kg Single injection, lasting 30 minutes To evaluate the effect of Prazosin on Ca2+ fluctuations in astrocytes during startle responses in mice. Results showed that Prazosin completely inhibited startle-induced Ca2+ fluctuations in astrocyte somata of WT mice, but did not alter the lack of Ca2+ fluctuations observed in the somata of IP3R2?/? mice. In astrocyte processes, Prazosin selectively inhibited the fast component of the startle-evoked Ca2+ event but had no effect on the late component. Nat Neurosci. 2015 May;18(5):708-17
C57BL/6 mice Cocaine-induced conditioned place preference model Intraperitoneal injection 1 mg/kg, 2 mg/kg Single dose, tested 30 minutes after administration To investigate the effects of Prazosin on cocaine-, stress-, and yohimbine-induced reinstatement. Results showed that Prazosin failed to block reinstatement induced by cocaine, stress, or yohimbine. Neuropsychopharmacology. 2010 Oct;35(11):2165-78

Prazosin HCl/哌唑嗪盐酸盐 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 <<

Prazosin HCl/哌唑嗪盐酸盐 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

Prazosin HCl/哌唑嗪盐酸盐 实验方案

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

Prazosin HCl/哌唑嗪盐酸盐 技术信息

CAS号19237-84-4
分子式C19H22ClN5O4
分子量 419.86
SMILES Code O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4=CC=CO4.Cl
MDL No. MFCD00058177
别名 盐酸哌唑嗪 ;Prazosin (hydrochloride); cp-12299-1; NSC 292810; Prazosin hydrochloride
运输蓝冰
InChI Key WFXFYZULCQKPIP-UHFFFAOYSA-N
Pubchem ID 68546
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Prazosin | 19237-84-4 | Adrenergic Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Autophagy | Adrenergic Receptor | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Prazosin HCl/哌唑嗪盐酸盐 纯度/质量文件 | Prazosin HCl/哌唑嗪盐酸盐 亚型比较 | Prazosin HCl/哌唑嗪盐酸盐 生物活性 | Prazosin HCl/哌唑嗪盐酸盐 临床数据 | Prazosin HCl/哌唑嗪盐酸盐 参考文献 | Prazosin HCl/哌唑嗪盐酸盐 实验方案 | Prazosin HCl/哌唑嗪盐酸盐 技术信息

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