Verapamil HCl
(Synonyms: 盐酸维拉帕米; (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride) 目录号 : GC17106
Verapamil HCl是 L 型钙通道阻滞剂和肾上腺素能受体拮抗剂，常用于高血压、心律失常和心绞痛的研究。
Cas No.:152-11-4
Sample solution is provided at 25 µL, 10mM.
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Verapamil HCl is an L-type calcium channel blocker and adrenergic receptor antagonist commonly used in studies of hypertension, arrhythmias and angina pectoris[1].
Verapamil HCl (5µM-5mM; 1h) affects human erythrocytes, where the normal disc-like shape of the erythrocytes changes to oropharyngeal cysts, small cells, spherical oropharyngeal cysts and haemolysis occurs at a concentration of Verapamil HCl of 5mM. As the concentration of Verapamil HCl was increased from 5µM, the morphology of the erythrocytes changed [2].The survival and proliferation rates of PC-3, A549, and COLO 205 cells were decreased after treatment with Verapamil HCl (50–200μM; 6–48h)[3] .
In the neuroinflammatory model, pretreatment with Verapamil HCl (10mg/kg; ip; 7days) in the morning reduced CD11b+, CD68+ and Iba1 by 54.33%, 24.68% and 41.33%, respectively. The above markers were also reduced in evening pretreated mice by 41.01%, 18.3% and 24.06%, respectively [4].Long-term administration of Verapamil HCl (200mg/kg; po; 10weeks) to mice rescued the lives of mice with myotonic dystrophy type 1 and improved myogenesis, muscle stiffness and respiratory function [5].Verapamil HCl (1.0, 2.5, 5.0 and 10mg/kg; ip; 48h) impaired memory consolidation in a parameter- and dose-dependent manner in an absent-field habituation task in rats [6].
References:
[1] Kania E, Pająk B, O'Prey J, Sierra Gonzalez P, Litwiniuk A, Urbańska K, Ryan KM, Orzechowski A. Verapamil HCl treatment induces cytoprotective autophagy by modulating cellular metabolism. FEBS J. 2017 May;284(9):1370-1387.
[2] Suwalsky M, Munoz M, Mennickent S, et al. Structural effects of Verapamil HCl on cell membranes and molecular models[J]. Journal of the Chilean Chemical Society, 2010, 55(1): 1-4.
[3] Mosalam EM, Elberri AI, Sallam AS, Salem HR, Metwally EM, Abdallah MS, Shaldam MA, Mansour HEA. Chronotherapeutic neuroprotective effect of Verapamil HCl against lipopolysaccharide-induced neuroinflammation in mice through modulation of calcium-dependent genes. Mol Med. 2022 Nov 26;28(1):139.
[4] Rattis BAC, Freitas AC, Oliveira JF, Calandrini-Lima JLA, Figueiredo MJ, Soave DF, Ramos SG, Celes MRN. Effect of Verapamil HCl, an L-Type Calcium Channel Inhibitor, on Caveolin-3 Expression in Septic Mouse Hearts. Oxid Med Cell Longev. 2021 Apr 8;2021:6667074.
[5]Cisco LA, Sipple MT, Edwards KM, Thornton CA, Lueck JD. Verapamil HCl mitigates chloride and calcium bi-channelopathy in a myotonic dystrophy mouse model. J Clin Invest. 2024 Jan 2;134(1):e173576.
[6]Popović N, Giménez de Béjar V, Caballero-Bleda M, Popović M. Verapamil HCl Parameter- and Dose-Dependently Impairs Memory Consolidation in Open Field Habituation Task in Rats. Front Pharmacol. 2017 Jan 10;7:539.
Verapamil HCl是 L 型钙通道阻滞剂和肾上腺素能受体拮抗剂，常用于高血压、心律失常和心绞痛的研究[1]。
Verapamil HCl （5µM-5mM；1h）影响人红细胞，在在 5mM 浓度的Verapamil HCl下，红细胞的正常圆盘状形状变为口咽囊肿、小细胞、球形口咽囊肿，并发生溶血。随着Verapamil HCl浓度从 5µM 增加，红细胞的形态发生变化 [2]。PC-3、A549 和 COLO 205 细胞存活率和增殖率在Verapamil HCl（50–200μM；6–48h）处理后降低 [3] 。
在神经炎症模型中，早晨给予Verapamil HCl (10mg/kg；ip ；7天 ) 预处理分别使 CD11b+、CD68+ 和 Iba1 降低 54.33%、24.68% 和 41.33%，晚上预处理小鼠的以上标志物也有降低，分别降低了 41.01%、18.3% 和 24.06%[4]。小鼠长期服用Verapamil HCl（200mg/kg； po； 10weeks）能挽救1型肌营养不良症小鼠的生命，并改善肌力生成、肌肉僵硬度和呼吸功能[5]。Verapamil HCl (1.0、2.5、5.0和10 mg/kg；ip；48h)在大鼠的旷场习惯任务中以参数和剂量依赖性的方式损害记忆巩固[6]。
| Cell experiment [1]: | |
Cell lines | SHSY5Y cells |
Preparation Method | SHSY5Y cells were seeded into 24-well plates . 2% FBS medium containing Verapamil HCl at a concentration range from 1nM to 0.5mM was added to the cells for 1, 6, 24 and 48h. Cell viability was assessed using the MTT reduction assay. |
Reaction Conditions | Verapamil HCl: 1nM -0.5mM; 6, 24 and 348h. |
Applications | A highly statistical reduction in cell viability was observed under 0.5mM Verapamil HCl treatment and was still not recovered after 48h; the other tested concentrations failed to produce any significant effects after 1, 6, and 24h. |
| Animal experiment [2]: | |
Animal models | Myotonic dystrophy mouse model |
Preparation Method | Mice were provided Verapamil HCl via ingestion of Nutra-Gel Complete Nutrition food to a final dose of 200mg/kg/day Verapamil HCl. Mice that did not receive Verapamil HCl, were provided Nutra-Gel Complete Nutrition food that had 1mL ddH2O added to serve as a vehicle control. |
Dosage form | Verapamil HCl (200mg/kg; po; 10weeks) |
Applications | Long-term administration of the calcium channel blocker Verapamil HClto mice rescued the life of mice with myotonic dystrophy type 1 and improved force production, muscle stiffness, and respiratory function. |
References: | |
| Cas No. | 152-11-4 | SDF | |
| 别名 | 盐酸维拉帕米; (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride | ||
| 化学名 | 2-(3,4-dimethoxyphenyl)-5-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]-2-propan-2-ylpentanenitrile;hydrochloride | ||
| Canonical SMILES | CC(C)C(CCCN(C)CCC1=CC(=C(C=C1)OC)OC)(C#N)C2=CC(=C(C=C2)OC)OC.Cl | ||
| 分子式 | C27H39ClN2O4 | 分子量 | 491.06 |
| 溶解度 | ≥ 14.45mg/mL in DMSO, ≥ 8.95 mg/mL in EtOH with ultrasonic, ≥ 6.41 mg/mL in Water with ultrasonic | 储存条件 | 4°C, protect from light |
| 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 | 2.0364 mL | 10.1821 mL | 20.3641 mL |
| 5 mM | 407.3 μL | 2.0364 mL | 4.0728 mL |
| 10 mM | 203.6 μL | 1.0182 mL | 2.0364 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；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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