标签归档：哌唑嗪

Prazosin hydrochloride(Synonyms: 哌唑嗪盐酸盐)

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Prazosin hydrochloride (Synonyms: 哌唑嗪盐酸盐) 纯度: 99.93%

Prazosin hydrochloride 是一种耐受良好、具有 CNS 活性的 α1-肾上腺素能受体(α1-adrenergic receptor) 拮抗剂。 可用于研究高血压和酒精使用障碍。 Prazosin hydrochloride 有效抑制去甲肾上腺素 (NE) 刺激的 45Ca 流出，IC50 为 0.15 nM。Prazosin hydrochloride 抑制有机阳离子转运蛋白 OCT-1 和 OCT-3，IC50 分别为 1.8 和 13 μM 。

Prazosin hydrochloride(Synonyms: 哌唑嗪盐酸盐)

Prazosin hydrochloride Chemical Structure

CAS No. : 19237-84-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥616 In-stock
100 mg ￥560 In-stock
200 mg ￥900 In-stock
500 mg ￥1800 In-stock
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5 g   询价  

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生物活性

Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders[1]. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM[2].Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively[3].

体外研究
(In Vitro)

Prazosin (0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 µM) effectively inhibits the proliferation of U251 and U87 cells[4].
Prazosin inhibits the migration and invasion of U251 and U87 cells[4].
Prazosin treatment decreases the protein expression of components of the PI3K/AKT/mTOR signaling pathway. Prazosin (13.16 and 11.57 µM for U251 and U87 cells, 48 hours) decreases the expression levels of P70 and cyclin D1, which are downstream target genes of the PI3K/AKT/mTOR signaling pathway[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: U251 and U87 cells
Concentration: 0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 µM.
Incubation Time: 48 hours
Result: The IC50s were 13.16±0.95 and 11.57±0.79 µM for U251 and U87 cells, respectively.

Western Blot Analysis

Cell Line: U251 and U87 cells
Concentration: 13.16 and 11.57 µM for U251 and U87 cells, respectively
Incubation Time: 48 hours
Result: Protein expression levels of Bax and active Caspase-3 were increased.
Bcl-2 levels were also decreased after prazosin treatment (P<0.05).
The expression of p-AKT and p-mTOR, P70 and cyclin D1 were decreased.

体内研究
(In Vivo)

Peripheral administration of Prazosin (0, 0.5, 1.0, 1.5 or 2.0 mg/kg; i.p.) can suppress not only central α1-adrenergic-mediated hyperexcitability but also stress-induced anxiety[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fifty-five alcohol-naive male rats from the 60th generation of selective breeding for alcohol preference[1]
Dosage: 0.5, 1.0, 1.5, or 2.0 mg/kg
Administration: Injected intraperitoneally (IP); 0.5 mg/mL; once a day at 15 min prior to onset of the daily two hour two-bottle choice, alcohol versus water, access period for two consecutive days and then three weeks later for five consecutive days.
Result: Significantly reduced alcohol intake during the initial two daily administrations, and this reduction of alcohol intake was maintained for five consecutive days by daily prazosin treatment in the subsequent more prolonged trial.

Clinical Trial

分子量

419.86

Formula

C19H22ClN5O4
CAS 号

19237-84-4
中文名称

哌唑嗪盐酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 14.29 mg/mL (34.04 mM; Need ultrasonic)

H2O : 0.59 mg/mL (1.41 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3817 mL 11.9087 mL 23.8175 mL
5 mM 0.4763 mL 2.3817 mL 4.7635 mL
10 mM 0.2382 mL 1.1909 mL 2.3817 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.43 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.43 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.43 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (3.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Dennis D Rasmussen, et al. The alpha1-adrenergic receptor antagonist, prazosin, reduces alcohol drinking in alcohol-preferring (P) rats. Alcohol Clin Exp Res. 2009 Feb;33(2):264-72.

    [2]. W S Colucci, et al. Nonlinear relationship between alpha 1-adrenergic receptor occupancy and norepinephrine-stimulated calcium flux in cultured vascular smooth muscle cells.Mol Pharmacol. 1985 May;27(5):517-24.

    [3]. Deborah L White, et al. OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.Blood. 2006 Jul 15;108(2):697-704.

    [4]. Jing Zhang, et al. Prazosin inhibits the proliferation, migration and invasion, but promotes the apoptosis of U251 and U87 cells via the PI3K/AKT/mTOR signaling pathway. Exp Ther Med. 2020 Aug;20(2):1145-1152.

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