Verapamil (hydrochloride)

Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research^[1][2][3]. IC50 & Target: Calcium channel^[1]
Permeability-glycoprotein (P-gp)^[1]
CYP3A4^[1] In Vitro: The EverFluor FL Verapamil (EFV) uptake by TR-iBRB2 cells is inhibited by cationic drugs, and inhibits by verapamil in a concentration-dependent manner with an IC₅₀ of 98.0 μM^[4]. In Vivo: Given orally Verapamil is useful for the prophylaxis of atrioventricular reentry tachycardia, and also in modulating the atrioventricular nodal response in atrial fibrillation^[2].
Verapamil is injected i.v. into a femoral vein prior to ischemia. Verapamil (1 mg/kg) significantly decreases the incidence of ventricular arrhythmias including premature ventricular contractions (PVC), ventricular tachycardia (VT) and ventricular fibrillation (VF) for 45-min coronary artery occlusion. Total arrhythmia scores are significantly increased when the heart is subjected to ischemia. Verapamil (1 mg/kg) significantly prevents the enhancement of total arrhythmia scores induced by ischemia^[5].