Description
Block L-type calcium channels in myocardial cells and vascular smooth muscle with Verapamil (Hydrochloride). Verapamil (Hydrochloride) binds to Cav1.2, a voltage-dependent L-type calcium channel, in a voltage- and frequency-dependent manner to inhibit calcium influx (Dilmac et al. Mol Pharmacol, 2004; Li & Shi. Pharmacol Res, 2019); IC50 values range from 250 nM - 15.5 μM (Hosey & Lazdunski. J Membr Biol, 1988). Widely expressed in vascular smooth muscle and myocardial cells, calcium influx through Cav1.2 channels propagates action potentials that produce muscle contraction (Ghosh et al. Vascul Pharmacol, 2017; Striessnig et al. Curr Mol Pharmacol, 2015). Verapamil (Hydrochloride) also interacts with other calcium and potassium channels and is an inhibitor of P-glycoprotein (Pauli-Magnus et al. J Pharmacol Exp Ther, 2000; Zhang et al. Circ Res, 1999).
Verapamil (Hydrochloride) has been used for:
CANCER RESEARCH
· Enhance the chemosensitivity of cancer cells to chemotherapeutic agents (Simpson. Cell Calcium, 1985; Wang et al. Oncol Rep, 2013).
· Improve the anti-tumor activity of an oncolytic adenovirus ICOVIR-5 in mouse xenograft models of lung cancer and melanoma (Gros et al. Mol Ther, 2010).
DISEASE MODELING
· Reduce arterial blood pressure values by inhibiting carbonic anhydrase I in human erythrocytes and vascular smooth muscles in animal models (Puscas et al. Cardiovasc Drugs Ther, 2000).
· Reduce pulse pressure and decrease carotid internal diameter, medial thickness, and collagen content in a rat model of spontaneous hypertension (Koffi et al. Am J Hypertens, 1999).
· Reduce the incidence of ventricular and total arrhythmias and reduce heart rate, arterial pressure, and left ventricular systolic pressure in a rat model (Zhou et al. PLoS One, 2013).
· Improve the cardiovascular pathology associated with Williams–Beuren syndrome in combination with curcumin in a mouse model (Abdalla et al. Int J Mol Sci, 2023).
