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]。