Verapamil is an L-type calcium channel blocker and adrenergic receptor antagonist commonly used in studies of hypertension, arrhythmias and angina pectoris[1].
Verapamil (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 of 5mM. As the concentration of Verapamil 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 (50–200μM; 6–48h)[3] .
In the neuroinflammatory model, pretreatment with Verapamil (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 (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 (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 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 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 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, 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 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 Parameter- and Dose-Dependently Impairs Memory Consolidation in Open Field Habituation Task in Rats. Front Pharmacol. 2017 Jan 10;7:539.
Verapamil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 （5µM-5mM；1h）影响人红细胞，在在 5mM 浓度的Verapamil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（50–200μM；6–48h）处理后降低 [3] 。
在神经炎症模型中，早晨给予Verapamil (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（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 (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]。