| CAS |
152-11-4 |
| Chinese Name |
盐酸维拉帕米 |
| English Name |
Verapamil Hydrochloride |
| Synonyms |
盐酸维拉帕米;戊脉安;棉籽糖;桉糖; |
| Molecular Formula |
C27H38N2O4·HCl |
| Molecular Weight |
491.07 |
| Solubility |
Soluble in DMSO ≥50mg/mL;Soluble in Ethanol ≥20mg/mL(Need ultrasonic) |
| Purity |
HPLC≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 205-800-5 |
| MDL |
MFCD00069355 |
| SMILES |
[H]Cl.COC1=CC=C(C(C#N)(C(C)C)CCCN(CCC2=CC=C(OC)C(OC)=C2)C)C=C1OC |
| InChIKey |
DOQPXTMNIUCOSY-UHFFFAOYSA-N |
| InChI |
InChI=1S/C27H38N2O4.ClH/c1-20(2)27(19-28,22-10-12-24(31-5)26(18-22)33-7)14-8-15-29(3)16-13-21-9-11-23(30-4)25(17-21)32-6;/h9-12,17-18,20H,8,13-16H2,1-7H3;1H |
| PubChem CID |
62969 |
| Target Point |
Calcium Channel;P-glycoprotein |
| Passage |
Membrane Transporter&Ion Channel;Neuronal Signaling |
| Background |
Verapamil Hydrochloride is considered as a calcium antagonist. |
| Biological Activity |
Verapamil hydrochloride 是钙离子通道 (calcium channel) 拮抗剂。[1-3] |
| In Vitro |
维拉帕米(盐酸盐)是L型钙通道拮抗剂。 Bortezomib和维拉帕米(70μM)的组合显著降低了培养16小时后JK-6L，RPMI 8226和ARH-77细胞系的活力[1]。重组人羧酸酯酶(CES2)的酶水解酶活性基本上被维拉帕米抑制，Ki为3.84±0.99μM[2]。 |
| In Vivo |
维拉帕米是一种钙通道拮抗剂，在缺血前静脉注射到股静脉中。维拉帕米(1 mg / kg)显着降低室性心律失常的发生率，包括室性心室收缩(PVC)，室性心动过速(VT)和45％冠状动脉闭塞的心室颤动(VF)。当心脏发生缺血时，总心律失常评分显着增加(与假手术相比，P <0.01)。维拉帕米(1mg / kg)显着阻止由缺血诱导的总心律失常评分的增强(P <0.01对比缺血)。结果表明维拉帕米具有抗心律失常作用[3]。 |
| Cell Experiment |
用10nM硼替佐米和/或70μM维拉帕米处理细胞(1×105)16小时，并用Alamar-Blue再孵育4小时。线粒体脱氢酶的活性导致着色的转换，然后使用分光光度计测量吸收[1]。 |
| Animal Experiment |
大鼠[3]使用成年雄性Sprague-Dawley(SD)大鼠(250-350g)。在缺血前10分钟将维拉帕米(1mg/kg)静脉内注射到股静脉中。假手术组经历了相同的外科手术，除了LAD下方的缝合线未被解开。在另一系列实验中，心律失常由Bay K8644(一种L型钙通道激动剂)以0.1mg/kg的剂量诱导进入FV。维拉帕米(1mg/kg)在Bay K8644之前10分钟施用。所有注射均在30秒内完成。 |
| Data Literature Source |
[1]. Meister S，et al. Calcium channel blocker Verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myeloma cells. Neoplasia. 2010 Jul;12(7):550-61.
[2]. Yanjiao X，et al. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468-74.
[3]. Zhou P，et al. Anti-arrhythmic effect of Verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013 Aug 12;8(8):e71567. |
| Unit |
Bottle |
| Specification |
10mg 10mM*1mL in DMSO 50mg |
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