Prazosin HCl
(Synonyms: 哌唑嗪盐酸盐) 目录号 : GC18072
Prazosin HCl是一种特异性的α1-肾上腺素能受体（α1-AR）的拮抗剂，与人类重组α1A-AR、α1B-AR和α1D-AR的结合常数（Ki值）分别为0.2、0.25和0.32nM，与α2-AR的Ki值分别为340和3.7nM（在表达α2A-AR 的 HT-29 细胞和表达α2B-AR 的 NG108 细胞中）。
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.
Prazosin HCl是一种特异性的α1-肾上腺素能受体（α1-AR）的拮抗剂，与人类重组α1A-AR、α1B-AR和α1D-AR的结合常数（Ki值）分别为0.2、0.25和0.32nM，与α2-AR的Ki值分别为340和3.7nM（在表达α2A-AR 的 HT-29 细胞和表达α2B-AR 的 NG108 细胞中） [1-2]。α1-AR属于七跨膜结构、与G蛋白偶联的受体超家族，位于中枢和外周神经系统中的α1-AR具有重要的治疗意义 [3]。Prazosin HCl可以抗炎、缓解焦虑、缓解恐慌，防止记忆衰退，调节阿片类药物的镇痛作用，可用于高血压和阿尔兹海默症研究 [4]。
在体外，Prazosin HCl（0, 2.5, 5, 7.5, 10, 15, 20, 30, 40, and 50μM; 24h）剂量依赖性地降低了MG63和143B细胞的活力，并显著减弱了细胞迁移和侵袭能力。Prazosin HCl通过下调Akt和mTOR磷酸化水平以及P70和细胞周期蛋白D1的表达来抑制Akt/mTOR通路 [5]。Prazosin HCl（30μM; 1h）预处理显著增加了多西紫杉醇诱导的PC-3和-LNCaP细胞的细胞毒性 [6]。
在体内，Prazosin HCl（1mg/kg/day; 两周; i.p.）治疗可预防阿兹海默病（AD）小鼠的记忆衰退，增加了小鼠的抗炎反应和星形胶质细胞活化，并显著增加了GFAP阳性细胞和神经元细胞数量 [1]。Prazosin HCl（0.01, 0.1, 0.25, 0.5, 1 and 2mg/kg/day; single-dose; i.p.）增强了吗啡对尾部拍击实验中小鼠的镇痛作用，而Prazosin HCl单独给药无镇痛作用 [7]。
| 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 | |
| 别名 | 哌唑嗪盐酸盐 | ||
| 化学名 | [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 | ||
| 分子式 | C19H21N5O4.HCl | 分子量 | 419.86 |
| 溶解度 | ≥ 7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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- Purity: >99.50%
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