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 。
| 生物活性 | Prazosin hydrochloride is a well-tolerated, CNS-activeα1-adrenergic receptorantagonist for the research of high blood pressure and alcohol use disorders[1]. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50of 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].
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. |
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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].
| Animal Model: | Fifty-five alcohol-naive male rats from the 60thgeneration 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. |
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| 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 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。
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