Prazosin HCl (Synonyms: CP 12,299-1, NSC 292810) |
رقم الكتالوجGC18072
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برازوسين حمض الهيدروكلوريك هو α جيد التحمل ونشط في الجهاز العصبي المركزي ؛ 1-adrenergic receptor antagonist لبحوث ارتفاع ضغط الدم واضطرابات تعاطي الكحول.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19237-84-4
Sample solution is provided at 25 µL, 10mM.
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Prazosin HCl is a specific antagonist of the α1-adrenergic receptor (α1-AR), with binding constants (Ki values) of 0.2, 0.25, and 0.32nM for human recombinant α1A-AR, α1B-AR, and α1D-AR, respectively, and 340 and 3.7nM for α2-AR (in HT-29 cells expressing α2A-AR and NG108 cells expressing α2B-AR) [1-2]. The α1-AR belongs to the seven-transmembrane structure and G protein-coupled receptor superfamily, and α1-AR located in the central and peripheral nervous systems have significant therapeutic significance [3]. Prazosin HCl can have anti-inflammatory effects, relieve anxiety, alleviate panic, prevent memory decline, and regulate the analgesic effect of opioid drugs, and can be used in the research of hypertension and Alzheimer's disease [4].
In vitro, Prazosin HCl (0, 2.5, 5, 7.5, 10, 15, 20, 30, 40, and 50μM; 24h) dose-dependently reduced the viability of MG63 and 143B cells and significantly weakened the cell migration and invasion ability. Prazosin HCl inhibits the Akt/mTOR pathway by down-regulating the phosphorylation levels of Akt and mTOR and the expression of P70 and cyclin D1 [5]. Prazosin HCl (30μM; 1h) pretreatment significantly increased the cytotoxicity of docetaxel-induced PC-3 and -LNCaP cells [6].
In vivo, Prazosin HCl (1mg/kg/day; 2 weeks; i.p.) treatment can prevent memory decline in Alzheimer's disease (AD) mice, increase the anti-inflammatory response and astrocyte activation of mice, and significantly increase the number of GFAP-positive cells and neuronal cells [1]. Prazosin HCl (0.01, 0.1, 0.25, 0.5, 1, and 2mg/kg/day; single-dose; i.p.) enhances the analgesic effect of morphine in mice in the tail flick test, while Prazosin HCl alone has no analgesic effect [7].
References:
[1] Katsouri L, Vizcaychipi MP, McArthur S, et al. Prazosin, an α(1)-adrenoceptor antagonist, prevents memory deterioration in the APP23 transgenic mouse model of Alzheimer's disease. Neurobiol Aging. 2013;34(4):1105-1115.
[2] Bylund DB, Ray-Prenger C. Alpha-2A and alpha-2B adrenergic receptor subtypes: attenuation of cyclic AMP production in cell lines containing only one receptor subtype. J Pharmacol Exp Ther. 1989;251(2):640-644.
[3] Sarma P K S, Tiwari A, Pal A. α1-Adrenoceptors as potential therapeutic targets[J]. Expert Opinion on Therapeutic Patents, 2005, 15(10): 1333-1351.
[4] Ozdoğan UK, Lähdesmäki J, Scheinin M. Influence of prazosin and clonidine on morphine analgesia, tolerance and withdrawal in mice. Eur J Pharmacol. 2003;460(2-3):127-134.
[5] An M, Ma W H, Jia H W, et al. Prazosin inhibits the growth and mobility of osteosarcoma cells[J]. Translational cancer research, 2019, 8(5): 1997.
[6] Spencer B H, McDermott C M, Chess-Williams R, et al. Prazosin but not tamsulosin sensitises PC-3 and LNCaP prostate cancer cells to docetaxel[J]. Pharmacology, 2018, 102(1-2): 17-25.
[7] Ozdoğan UK, Lähdesmäki J, Scheinin M. Influence of prazosin and clonidine on morphine analgesia, tolerance and withdrawal in mice. Eur J Pharmacol. 2003;460(2-3):127-134.
| Cell experiment [1]: | |
Cell lines | MG63 and 143B cells |
Preparation Method | Cells were cultured in Dulbecco’s Modified Eagle Medium (DMEM) medium supplemented with 10% fetal bovine serum (FBS) at 37 °C with 5% CO2. The cells were treated with different concentrations of Prazosin HCl (0, 2.5, 5, 7.5, 10, 15, 20, 30, 40, and 50µM), with Prazosin’s effect on cell viability being analyzed by CCK8 assay. After treatment for 24h, cells were cultured with CCK8 reagent (10µL/well) at 37°C for 90min with absorbance being measured at 450nm. |
Reaction Conditions | 0, 2.5, 5, 7.5, 10, 15, 20, 30, 40, and 50μM; 24h |
Applications | Prazosin HCl dose-dependently reduced the viability of MG63 and 143B cells. |
| Animal experiment [2]: | |
Animal models | C57 Bl/6 J mice |
Preparation Method | Each mouse was tested only once. The group n was 9 to 10. The basal tail-flick scores were first measured followed by a second tail-flick measurement 30min after i.p. administration of the test drugs (Prazosin HCl 0.01, 0.1, 0.25, 0.5, 1 or 2mg/kg, or clonidine 5mg/kg, or cirazoline 0.3mg/kg, or corynanthine 0.5mg/kg, or saline). Then, a 5mg/kg test dose of morphine was administered to all mice, and 30min later, tail-flick scores were measured for the third time. Tail-flick scores were converted to %MPE (Maximal Possible Effect): %MPE=(measured tail-flick score—average tail-flick score of saline-treated control group)/(cutoff time—average tail-flick score of saline-treated control group)×100%. |
Dosage form | 0.01, 0.1, 0.25, 0.5, 1 and 2mg/kg/day; single-dose; i.p. |
Applications | Prazosin HCl enhances the analgesic effect of morphine in the tail flick test in mice, while Prazosin HCl given alone has no analgesic effect. |
References: | |
| Cas No. | 19237-84-4 | SDF | |
| المرادفات | CP 12,299-1, NSC 292810 | ||
| Chemical Name | [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(furan-2-yl)methanone;hydrochloride | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4=CC=CO4)N)OC.Cl | ||
| Formula | C19H21N5O4.HCl | M.Wt | 419.86 |
| الذوبان | ≥ 7mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3817 mL | 11.9087 mL | 23.8175 mL |
| 5 mM | 476.3 μL | 2.3817 mL | 4.7635 mL |
| 10 mM | 238.2 μL | 1.1909 mL | 2.3817 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)