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拉西地平

拉西地平用途

【用途一】
血管选择性钙拮抗剂，具有高效和长效的降压活性。用于高血压。
【用途二】
治疗高血压。

拉西地平名称

[ CAS 号 ]:
103890-78-4

[ 中文名 ]:
拉西地平

[ 英文名 ]:
Lacidipine

[中文别名 ]:

[英文别名 ]:

Caldine
Lacipil
MFCD00865936
Lacirex
Lacidipine
Motens

拉西地平生物活性

[ 描述 ]:

Lacidipine (Lacipil, Motens)是L型钙离子通道阻断剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 心血管疾病

[参考文献]

[1]. Zhang, A., et al., Lacidipine attenuates apoptosis via a caspase-3 dependent pathway in human kidney cells. Cell Physiol Biochem, 2013. 32(4): p. 1040-9.

[2]. van Amsterdam, F.T., et al., Lacidipine: a dihydropyridine calcium antagonist with antioxidant activity. Free Radic Biol Med, 1992. 12(3): p. 183-7.

[3]. Kamal, S.M., Possible hepatoprotective effects of lacidipine in irradiated DOCA-salt hypertensive albino rats. Pak J Biol Sci, 2013. 16(21): p. 1353-7.

[相关活性小分子]

拉西地平物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
558.4±50.0 °C at 760 mmHg

[ 熔点 ]:
174-175°C

[ 分子式 ]:
C₂₆H₃₃NO₆

[ 分子量 ]:
455.543

[ 闪点 ]:
291.5±30.1 °C

[ 精确质量 ]:
455.230774

[ PSA ]:
90.93000

[ LogP ]:
5.49

[ 外观性状 ]:
白色至灰白色结晶固体

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.540

[ 储存条件 ]:
-20?C Freezer

拉西地平MSDS

详细MSDS(安全技术说明书)

拉西地平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US7970200

CHEMICAL NAME :: 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-(3-(1,1-dimethylethoxy) -3-oxo-1- propenyl)phenyl)-, diethyl ester, (E)-

CAS REGISTRY NUMBER :: 103890-78-4

LAST UPDATED :: 199410

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C26-H33-N-O6

MOLECULAR WEIGHT :: 455.60

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 880 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43300 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 562 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3150 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 80200 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Skin and Appendages - hair

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 291 mg/kg/1Y-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Endocrine - changes in adrenal weight Endocrine - changes in thymus weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,343,1994 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1260 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,377,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 52 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,399,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 234 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,389,1994

拉西地平安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
C,Xi

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S45

[ 危险品运输编码 ]:
UN 3265 8/PG 2

[ WGK德国 ]:
3

[ 包装等级 ]:
III

[ 危险类别 ]:
8

[ 海关编码 ]:
2933399090

拉西地平合成路线

详细合成路线

拉西地平上下游产品

拉西地平上游产品

拉西地平下游产品

拉西地平制备

【方法一】
邻苯二甲醛和三苯膦乙酸叔丁酯在二氯甲烷中，于0℃反应15min，得3-(2-甲酰基苯基)丙烯酸叔丁酯。再和2-氨基-2-丁烯酸乙酯，在乙酸中，在室温下反应5h而得。

拉西地平海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

拉西地平文献

Possible hepatoprotective effects of lacidipine in irradiated DOCA-salt hypertensive albino rats.

Pak. J. Biol. Sci. 16(21) , 1353-7, (2013)

Calcium channel blockers are increasingly used for the treatment of hypertension. Hypertension is an important risk factor for liver damage and several other circulatory abnormalities. The aim of this...

Effect of long-term antihypertensive treatment on white-coat hypertension.

Hypertension 64(6) , 1388-98, (2014)

Limited evidence is available on the extent and frequency by which antihypertensive treatment lowers office blood pressure (BP) in white-coat hypertension (WCH). Data are even more scanty and discrepa...

Ordered mesoporous silica material SBA-15: loading of new calcium channel blocker--lacidipine.

J. Microencapsul. 30(1) , 21-7, (2013)

Mesoporous material SBA-15 of hexagonal structure was synthesised and its usefulness as a carrier for a poorly soluble drug--lacidipine (LA)--was tested. The source of silica was tetraethyl orthosilic...

更多文献