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盐酸维拉帕米

盐酸维拉帕米用途

Verapamil hydrochloride 是钙离子通道 (calcium channel) 拮抗剂。

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盐酸维拉帕米名称

[ CAS 号 ]:
152-11-4

[ 中文名 ]:
盐酸维拉帕米

[ 英文名 ]:
Verapamil HCl

[中文别名 ]:

[英文别名 ]:

MFCD00069355
Izoptin Hydrochloride
(±)-Verapamil hydrochloride
Verogalid ER
dl-Verapamil Hydrochloride
Veraptin
Arpamyl
Veracim
Verapamil hydrochloride
(‘±)-Verapamil hydrochloride

盐酸维拉帕米生物活性

[ 描述 ]:

Verapamil hydrochloride 是钙离子通道 (calcium channel) 拮抗剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 心血管疾病

[ 靶点 ]

Calcium channel[1]

[体外研究]

维拉帕米(盐酸盐)是L型钙通道拮抗剂。 Bortezomib和维拉帕米(70μM)的组合显着降低了培养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]。

[体内研究]

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]。

[细胞实验]

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]。

[动物实验]

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。

[参考文献]

[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.

[相关活性小分子]

盐酸维拉帕米物理化学性质

[ 密度 ]:
1.058g/cm3

[ 沸点 ]:
586.1ºC at 760 mmHg

[ 熔点 ]:
142 °C (dec.)(lit.)

[ 分子式 ]:
C₂₇H₃₉ClN₂O₄

[ 分子量 ]:
491.063

[ 闪点 ]:
308.3ºC

[ 精确质量 ]:
490.259827

[ PSA ]:
63.95000

[ LogP ]:
5.89508

[ 外观性状 ]:
白色至灰白色粉末

[ 储存条件 ]:
Refrigerator (+4°C)

[ 水溶解性 ]:
soluble

盐酸维拉帕米MSDS

详细MSDS(安全技术说明书)

盐酸维拉帕米毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YV8320000

CHEMICAL NAME :: Valeronitrile, 5-((3,4-dimethoxyphenethyl)methylamino)-2-(3,4-dimeth oxyphenyl)-2-isopropy l-, monohydrochloride

CAS REGISTRY NUMBER :: 152-11-4

LAST UPDATED :: 199707

DATA ITEMS CITED :: 32

MOLECULAR FORMULA :: C27-H38-N2-O4.Cl-H

MOLECULAR WEIGHT :: 491.13

WISWESSER LINE NOTATION :: 1OR BO1 DXCNY1&1&3N1&2R CO1 DO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 96 mg/kg

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - acute pulmonary edema

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 72 mg/kg/14H-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 58 mg/kg

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - acute pulmonary edema

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 80 mg/kg

TOXIC EFFECTS :: Behavioral - coma Cardiac - pulse rate Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 89 mg/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Vascular - BP lowering not characterized in autonomic section Nutritional and Gross Metabolic - changes in calcium

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 14400 ug/kg

TOXIC EFFECTS :: Vascular - regional or general arteriolar constriction

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3429 ug/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Gastrointestinal - necrotic changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 135 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - coma Lungs, Thorax, or Respiration - cyanosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 26 mg/kg

TOXIC EFFECTS :: Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 143 ug/kg/4H-C

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 68571 mg/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Cardiac - pulse rate Vascular - regional or general arteriolar or venous dilation

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 71 ug/kg/5M-C

TOXIC EFFECTS :: Behavioral - excitement Cardiac - arrhythmias (including changes in conduction) Cardiac - pulse rate increase, without fall in BP

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 1026 ug/kg

TOXIC EFFECTS :: Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 200 ug/kg/15S-C

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 256 ug/kg/1H-I

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 108 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 107 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 16 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 47 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 163 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 41 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 68 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5795 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Gastrointestinal - hypermotility, diarrhea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 140 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 128 mg/kg

SEX/DURATION :: male 28 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - impotence

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 264 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception lactating female 22 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow)

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 30 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 244,135,1990 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5040 No. of Facilities: 174 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 3974 (estimated) No. of Female Employees: 2638 (estimated)

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盐酸维拉帕米安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301 + H311 + H331

[ 警示性声明 ]:
P261-P280-P301 + P310-P311

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25

[ 安全声明 (欧洲) ]:
S45-S36/37/39-S36/37

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
YV8320000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2926909090

盐酸维拉帕米制备

由愈创木酚为原料制得。

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盐酸维拉帕米海关

[ 海关编码 ]: 2926909090

[ 中文概述 ]:
2926909090 其他腈基化合物. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
HS:2926909090 other nitrile-function compounds VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

盐酸维拉帕米文献

Utility of cerebrospinal fluid drug concentration as a surrogate for unbound brain concentration in nonhuman primates.

Drug Metab. Pharmacokinet. 29(5) , 419-26, (2014)

In central nervous system drug discovery, cerebrospinal fluid (CSF) drug concentration (C(CSF)) has been widely used as a surrogate for unbound brain concentrations (C(u,brain)). However, previous rod...

Salt effects in electromembrane extraction.

J. Chromatogr. A. 1347 , 1-7, (2014)

Electromembrane extraction (EME) was performed on samples containing substantial amounts of NaCl to investigate how the presence of salts affected the recovery, repeatability, and membrane current in ...

In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.

J. Biol. Chem. 288(47) , 33585-97, (2013)

We report that a localized intracellular and extracellular Ca(2+) mobilization occurs at the site of microscopic epithelial damage in vivo and is required to mediate tissue repair. Intravital confocal...

更多文献

盐酸维拉帕米

盐酸维拉帕米用途

盐酸维拉帕米名称

盐酸维拉帕米生物活性

盐酸维拉帕米物理化学性质

盐酸维拉帕米MSDS

详细MSDS(安全技术说明书)

盐酸维拉帕米毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

盐酸维拉帕米安全信息

盐酸维拉帕米制备

盐酸维拉帕米海关

盐酸维拉帕米文献

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