Nadolol是一种非选择性、口服有效的β-肾上腺素能拮抗剂，具有抗高血压和抗心律失常活性。
Cas No.:42200-33-9
Sample solution is provided at 25 µL, 10mM.
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Nadolol is a non-selective and orally active beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities [1]. Nadolol can inhibit the calmodulin-activated Ca2+-ATPase of human erythrocyte membranes [2]. Nadolol has been widely used to reduce heart rate at rest and during exercise and to reduce plasma renin activity[3].
In vitro, Nadolol treatment (10µM) for 24 hours significantly increased Gαs protein levels and enhanced basal cAMP levels in β2AR-expressing HEK 293 cells[4]. Treatment with 250µM Nadolol for 48h induced apoptosis and decreased mitochondrial membrane potential in A549 cells[5].
In vivo, Nadolol treatment via intraperitoneal injection at a single dose of 20mg/kg significantly reduced the number and area of lung metastases in a B16F10 cell-xenograft mouse model under acute social stress during 15 days[6]. A single dose of 5mg/kg Nadolol was injected intraperitoneally at 1h after reperfusion, which significantly reversed the increases in neurological deficit score and infarct volume in the ischemic stroke rats[7].
References:
[1] Kalsoom S, Zamir A, Rehman A U, et al. Clinical pharmacokinetics of nadolol: A systematic review[J]. Journal of Clinical Pharmacy and Therapeutics, 2022, 47(10): 1506-1516.
[2] Meltzer H L, Kassir S. Inhibition of calmodulin-activated Ca2+-ATPase by propranolol and nadolol[J]. Biochimica et Biophysica Acta (BBA)-General Subjects, 1983, 755(3): 452-456.
[3] Heel R C, Brogden R N, Pakes G E, et al. Nadolol: a review of its pharmacological properties and therapeutic efficacy in hypertension and angina pectoris[J]. Drugs, 1980, 20(1): 1-23.
[4] Peng H, Bond R A, Knoll B J. The effects of acute and chronic nadolol treatment on β2AR signaling in HEK293 cells[J]. Naunyn-Schmiedeberg's archives of pharmacology, 2011, 383(2): 209-216.
[5] Kavakcıoğlu Yardımcı B, Geyikoglu F, Aysin F, et al. The cytotoxic and apoptotic effects of beta-blockers with different selectivity on cancerous and healthy lung cell lines[J]. Molecular Biology Reports, 2021, 48(5): 4009-4019.
[6] Vegas O, Garmendia L, Arregi A, et al. Effects of antalarmin and nadolol on the relationship between social stress and pulmonary metastasis development in male OF1 mice[J]. Behavioural brain research, 2009, 205(1): 200-206.
[7] Yang X Y, Zhu W J, Chen D, et al. Nadolol Attenuates Brain Cell Ferroptosis in Ischemic Stroke Rats by Targeting the HOIL-1/IRP2 Pathway[J]. CNS & Neurological Disorders-Drug Targets, 2025, 24(5): 397-408.
Nadolol是一种非选择性、口服有效的β-肾上腺素能拮抗剂，具有抗高血压和抗心律失常活性[1]。Nadolol可抑制人红细胞膜钙调蛋白激活的Ca2+-ATP酶[2]。Nadolol已被广泛用于降低静息和运动时的心率，并降低血浆肾素活性[3]。
在体外，使用10µM的Nadolol处理表达β2AR的HEK 293细胞24小时，显著增加了Gαs蛋白水平并增强了基础cAMP水平[4]。使用250µM的Nadolol处理48小时，诱导了A549细胞凋亡并降低了线粒体膜电位 [5]。
在体内，在急性社会应激期间，单次腹腔注射20mg/kg的Nadolol，显著减少了B16F10细胞异种移植小鼠模型中的肺转移灶数量和面积（持续15天）[6]。再灌注后1小时单次腹腔注射5mg/kg的Nadolol，显著逆转了缺血性卒中大鼠的神经功能缺损评分和梗死体积的增加[7]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were cultured in DMEM/F12 medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). A549 cells (1×104 per well) were inoculated in a 96-well cell culture plate and incubated at 37°C with 5% CO2 for 24h. Then, the cells were treated with different concentrations of Nadolol (5, 10, 25, 50, 100, 150, 200, and 250µM) for 48h, respectively, and cell viability was measured. |
Reaction Conditions | 5, 10, 25, 50, 100, 150, 200, and 250µM; 48h |
Applications | Nadolol treatment reduced the cell viability of A549 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley (SD) rats |
Preparation Method | Male Sprague-Dawley (SD) rats (250-300g) were housed in groups of 3-5 rats per cage with free access to food and water ad libitum. The 12-h light/dark cycles were maintained throughout the duration of animal housing, with light periods beginning consistently at 7:00 am. Before surgery, the rats were fasted overnight but were free to drink tap water. The ischemic stroke rat model was constructed by Middle Cerebral Artery Occlusion (MCAO). Rats were randomly distributed into four groups (n=12 per group): (1) the sham group, (2) the stroke group, (3) the stroke+Nadolol group, rats received Nadolol (5mg/kg; i.p.) at 1h after reperfusion, and (4) the stroke+vehicle group, rats received DMSO (i.p.) at 1h after reperfusion. Following the end of reperfusion, an assessment of the neurological deficit score was first conducted, and then the rats were executed under anesthesia. The brain tissues were preserved for infarct volume measurement. |
Dosage form | 5mg/kg for once; i.p. |
Applications | Nadolol treatment reversed the increases in neurological deficit score and infarct volume in the ischemic stroke rats. |
References: | |
| Cas No. | 42200-33-9 | SDF | |
| 别名 | 纳多洛尔; SQ-11725 | ||
| Canonical SMILES | OC1CC2=C(C(OCC(O)CNC(C)(C)C)=CC=C2)CC1O | ||
| 分子式 | C17H27NO4 | 分子量 | 309.4 |
| 溶解度 | Methanol: 250 mg/mL (808.02 mM) | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2321 mL | 16.1603 mL | 32.3206 mL |
| 5 mM | 646.4 μL | 3.2321 mL | 6.4641 mL |
| 10 mM | 323.2 μL | 1.616 mL | 3.2321 mL |
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| 给药剂量 | mg/kg |  |
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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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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