Prazosin is an α-adrenergic receptor antagonist. Prazosin can reduce inflammation, relieve anxiety, alleviate panic, prevent memory decline, and modulate the pain-relieving effects of opioids. Prazosin can be used in the study of hypertension and Alzheimer’s disease.
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Prazosin Chemical Structure
CAS No. :
19216-56-9
This product is a controlled substance and not for sale in your territory.
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 is an α-adrenergic receptor antagonist. Prazosin can reduce inflammation, relieve anxiety, alleviate panic, prevent memory decline, and modulate the pain-relieving effects of opioids. Prazosin can be used in the study of hypertension and Alzheimer’s disease[1][2][3][4].
Cellular Effect
Cell Line
Type
Value
Description
References
HEK293
IC50
0.88 nM
Compound: prazosin
Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells after 60 mins
Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells after 60 mins
[PMID: 23403082]
HEK293
IC50
1.6 μM
Compound: prazosin
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293
IC50
13.6 μM
Compound: prazosin
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
[PMID: 23241029]
HEK293
IC50
38.4 μM
Compound: prazosin
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293
IC50
9.9 μM
Compound: prazosin
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
LNCaP
IC50
67.46 μM
Compound: 1
Antiproliferative activity was determined by colorimetric MTS assay in LNCaP cells after 72 hr of incubation with compounds (1-100 uM)
Antiproliferative activity was determined by colorimetric MTS assay in LNCaP cells after 72 hr of incubation with compounds (1-100 uM)
[PMID: 15633998]
PC-3
IC50
11.72 μM
Compound: Prazosin
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
[PMID: 33160761]
In Vitro
Prazosin (50 μM, 18 h) can reduce the production of amyloid beta in N2a cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Prazosin Related Antibodies
Western Blot Analysis[2]
Cell Line:
N2asw
Concentration:
50 μM
Incubation Time:
18 h
Result:
Reduced Aβ levels, induced a significant increase in APP-CTFs, and significantly reduced the production of CTFγ.
In Vivo
Prazosin (1 mg/kg, injected into the abdomen once daily, two weeks) can prevent memory deficits in mice by altering the release of inflammatory mediators and astrocytes, alleviating symptoms of Alzheimer's disease[2].
Prazosin (0.1-2 mg/kg, 3-6 mM, administered systemically or locally, in a single dose) can promote fear extinction in mice[3].
Prazosin (0.01-1 mg/kg, subcutaneously, in a single dose) can enhance the analgesic effects of morphine in mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
APP23 mice[2]
Dosage:
1 mg/kg; daily; 2 weeks
Administration:
Intraperitoneal injection (i.p.)
Result:
Increased mean freezing time during acclimation, attenuated hippocampal-dependent memory decline, did not affect APP processing or Aβ aggregation in vivo, and increased the number of astrocytes and secretion of anti-inflammatory mediators in APP23 mice.
Animal Model:
C57B1/6N mouse[3]
Dosage:
0.1-2 mg/kg; 3 and 6 mM; single dose
Administration:
systemic (0.1-2 mg/kg) or local microinjections (3 or 6 mM) into the prelimbic division of medial prefrontal cortex or basolateral amygdala
Result:
Had no effect on fear memory, but indirectly promoted fear extinction by interfering with the initial fear acquisition process.
Animal Model:
C57BL/6J mice[4]
Dosage:
0.01, 0.1, 0.25, 0.5, 1 mg/kg; single dose
Administration:
Subcutaneous injection (s.c.)
Result:
Had no analgesic effect when used alone, but it enhanced the analgesic effect of morphine and reduced weight loss after morphine withdrawal.
DMSO : 41.67 mg/mL (108.69 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.6082 mL
13.0412 mL
26.0824 mL
5 mM
0.5216 mL
2.6082 mL
5.2165 mL
10 mM
0.2608 mL
1.3041 mL
2.6082 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (50.0 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.
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]. Day HE, et al. Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord. J Chem Neuroanat. 1997 Jul;13(2):115-39.
[Content Brief]
[2]. Loukia Katsouri, et al. Prazosin, an α(1)-adrenoceptor antagonist, prevents memory deterioration in the APP23 transgenic mouse model of Alzheimer's disease. Neurobiol Aging. 2013 Apr;34(4):1105-15.
[Content Brief]
[3]. Elizabeth K Lucas, et al. Prazosin during fear conditioning facilitates subsequent extinction in male C57Bl/6N mice. Psychopharmacology (Berl). 2019 Jan;236(1):273-279.
[Content Brief]
[4]. Umit Kazim Ozdoğan, et al. Influence of prazosin and clonidine on morphine analgesia, tolerance and withdrawal in mice. Eur J Pharmacol. 2003 Jan 24;460(2-3):127-34.
[Content Brief]
[1]. Day HE, et al. Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord. J Chem Neuroanat. 1997 Jul;13(2):115-39.
[2]. Loukia Katsouri, et al. Prazosin, an α(1)-adrenoceptor antagonist, prevents memory deterioration in the APP23 transgenic mouse model of Alzheimer's disease. Neurobiol Aging. 2013 Apr;34(4):1105-15.
[3]. Elizabeth K Lucas, et al. Prazosin during fear conditioning facilitates subsequent extinction in male C57Bl/6N mice. Psychopharmacology (Berl). 2019 Jan;236(1):273-279.
[4]. Umit Kazim Ozdoğan, et al. Influence of prazosin and clonidine on morphine analgesia, tolerance and withdrawal in mice. Eur J Pharmacol. 2003 Jan 24;460(2-3):127-34.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.6082 mL
13.0412 mL
26.0824 mL
65.2061 mL
5 mM
0.5216 mL
2.6082 mL
5.2165 mL
13.0412 mL
10 mM
0.2608 mL
1.3041 mL
2.6082 mL
6.5206 mL
15 mM
0.1739 mL
0.8694 mL
1.7388 mL
4.3471 mL
20 mM
0.1304 mL
0.6521 mL
1.3041 mL
3.2603 mL
25 mM
0.1043 mL
0.5216 mL
1.0433 mL
2.6082 mL
30 mM
0.0869 mL
0.4347 mL
0.8694 mL
2.1735 mL
40 mM
0.0652 mL
0.3260 mL
0.6521 mL
1.6302 mL
50 mM
0.0522 mL
0.2608 mL
0.5216 mL
1.3041 mL
60 mM
0.0435 mL
0.2174 mL
0.4347 mL
1.0868 mL
80 mM
0.0326 mL
0.1630 mL
0.3260 mL
0.8151 mL
100 mM
0.0261 mL
0.1304 mL
0.2608 mL
0.6521 mL
Prazosin Related Classifications
EndocrinologyCardiovascular Disease
GPCR/G ProteinNeuronal Signaling
Adrenergic Receptor
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.