Verapamil

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Chemical Structure| 52-53-9 同义名 : CP-16533-1; (±)-Verapamil; NSC 135784
CAS号 : 52-53-9
货号 : A149080
分子式 : C27H38N2O4
纯度 : 98%
分子量 : 454.6
MDL号 : MFCD00056240
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(230.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Verapamil is a calcium channel blocker. Intravenous verapamil is highly effective in the termination of paroxysmal reciprocating atrioventricular tachycardia, whether associated with preexcitation or involving the atrioventricular node alone. Given orally it is useful for the prophylaxis of atrioventricular reentry tachycardia, and also in modulating the atrioventricular nodal response in atrial fibrillation[4]. 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[5]. Approximately 80 percent of patients with PSVT will convert to normal sinus rhythm after verapamil 0.075-0.15 mg/kg. Atrial fibrillation and flutter seldom convert to sinus rhythm with verapamil, but it successfully reduces the ventricular rate in 90 percent of these patients. Verapamil is useful for the rapid conversion of PSVT to normal sinus rhythm and for the rapid control of ventricular rate in atrial fibrillation and flutter before other antiarrhythmics have taken effect[6]. 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. 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[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.00mL

4.40mL

2.20mL
参考文献

[1]Popović N, Morales-Delgado N, Vidal Mena D, Alonso A, Pascual Martínez M, Caballero Bleda M, Popović M. Verapamil and Alzheimer's Disease: Past, Present, and Future. Front Pharmacol. 2020 May 5;11:562.

[2]Jangholi E, Sharifi ZN, Hoseinian M, Zarrindast MR, Rahimi HR, Mowla A, Aryan H, Javidi MA, Parsa Y, Ghaffarpasand F, Yadollah-Damavandi S, Arani HZ, Shahi F, Movassaghi S. Verapamil Inhibits Mitochondria-Induced Reactive Oxygen Species and Dependent Apoptosis Pathways in Cerebral Transient Global Ischemia/Reperfusion. Oxid Med Cell Longev. 2020 Oct 17;2020:5872645.

[3]Al-Sandaqchi AT, Marsh V, Williams HEL, Stevenson CW, Elsheikha HM. Structural, Functional, and Metabolic Alterations in Human Cerebrovascular Endothelial Cells during Toxoplasma gondii Infection and Amelioration by Verapamil In Vitro. Microorganisms. 2020 Sep 10;8(9):1386.

[4]Krikler DM. Verapamil in arrhythmia. Br J Clin Pharmacol. 1986;21 Suppl 2(Suppl 2):183S-189S

[5]Kubo Y, Nakazawa A, Akanuma SI, Hosoya KI. Blood-to-Retina Transport of Fluorescence-Labeled Verapamil at the Blood-Retinal Barrier. Pharm Res. 2018 Mar 12;35(5):93

[6]McMahon MT, Sheaffer SL. Verapamil (Isoptin, Knoll; Calan, Searle). Drug Intell Clin Pharm. 1982 Jun;16(6):443-7

[7]Zhou P, Zhang SM, Wang QL, Wu Q, Chen M, Pei JM. Anti-arrhythmic effect of verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013 Aug 12;8(8):e71567