Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
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Prazosin hydrochloride Chemical Structure
CAS No. : 19237-84-4
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The expression of TNS1 in U937 and HL60 cells treated with different concentration of Prazosin is detected by Western blot analysis
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α adrenergic receptor β adrenergic receptor
Description
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].
IC50 & Target
α adrenergic receptor
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Prazosin hydrochloride Related Antibodies
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.
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].
MedChemExpress (MCE) 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.
DMSO : 14.29 mg/mL (34.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.59 mg/mL (1.41 mM; Need ultrasonic)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (14.3 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[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.
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O / DMSO
1 mM
2.3817 mL
11.9087 mL
23.8175 mL
59.5437 mL
DMSO
5 mM
0.4763 mL
2.3817 mL
4.7635 mL
11.9087 mL
10 mM
0.2382 mL
1.1909 mL
2.3817 mL
5.9544 mL
15 mM
0.1588 mL
0.7939 mL
1.5878 mL
3.9696 mL
20 mM
0.1191 mL
0.5954 mL
1.1909 mL
2.9772 mL
25 mM
0.0953 mL
0.4763 mL
0.9527 mL
2.3817 mL
30 mM
0.0794 mL
0.3970 mL
0.7939 mL
1.9848 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Prazosin hydrochloride Related Classifications
GPCR/G ProteinNeuronal SignalingAutophagy
Adrenergic ReceptorAutophagy
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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