品牌现货直购
供应商:我要出现这里



查看所有供应商和价格请点击:

86780-90-7生产厂家

86780-90-7价格

86780-90-7

86780-90-7结构式
86780-90-7结构式

化源商城直购

中文名 阿雷地平
英文名 3-O-methyl 5-O-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
中文别名 2,6-二甲基-4-(2-硝基苯基)-1,4-二氢-3,5-吡啶二羧酸甲基2-氧丙基酯
英文别名 Sapresta
aranidipine
Mpc-1304
MPC1304
描述 MPC1304 是一种钙离子 (Ca2+) 通道拮抗剂,具有强大而持久的抗高血压作用。
相关类别
靶点

Ca2+ Channel [1]

体内研究 MPC1304(MPC-1304)是自发性高血压大鼠中新的Ca2 +通道拮抗剂。口服给予自发性高血压大鼠(SHR)剂量为3和10 mg/kg的MPC1304后,与对照组相比,特异性[3H](+)- PN 200-110与心肌膜结合的Bmax值显着降低。值。与对照值相比,1小时(3mg/kg),1小时和6小时(10mg/kg)的Bmax值显着降低(分别为47.7,48.9和25.8%)。效果在1小时时最大,并随时间降低。口服MPC1304后6小时(3mg/kg)和12或24小时(10mg/kg)的Bmax值与对照值没有显着差异,表明MPC1304的作用消失。心肌[3H](+)- PN 200-110结合的Kd值通过口服MPC1304未改变[1]。
动物实验 大鼠[1]使用雄性SHR(11-15周)。在给药前禁食16小时,并通过胃管口服MPC1304(3,10mg / kg)。对照动物给予载体。在给药后1-24小时,在用乙醚轻度麻醉下通过降主动脉的出血杀死SHR,并且用来自主动脉的0.9%盐水灌注心肌和脑。然后,移除两个组织,并修剪掉血管。通过离心分离来自大鼠血液的血浆,并储存在-80℃直至测定MPC1304的浓度。
参考文献

[1]. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneously hypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6.

密度 1.284 g/cm3
沸点 530ºC at 760 mmHg
熔点 155°
分子式 C19H20N2O7
分子量 388.37100
闪点 274.3ºC
精确质量 388.12700
PSA 127.52000
LogP 2.98680
折射率 1.555
储存条件 -20°C,密闭,干燥
分子结构

1、 摩尔折射率:87.90

2、 摩尔体积(cm3/mol):272.2

3、 等张比容(90.2K):709.4

4、 表面张力(dyne/cm):46.0

5、 极化率(10-24cm3):34.84

计算化学

1.疏水参数计算参考值(XlogP):无

2.氢键供体数量:1

3.氢键受体数量:8

4.可旋转化学键数量:7

5.互变异构体数量:15

6.拓扑分子极性表面积128

7.重原子数量:28

8.表面电荷:0

9.复杂度:748

10.同位素原子数量:0

11.确定原子立构中心数量:0

12.不确定原子立构中心数量:1

13.确定化学键立构中心数量:0

14.不确定化学键立构中心数量:0

15.共价键单元数量:1

更多

1.性状:从乙酸乙酯-己烷得黄色棱状结晶。

2.熔点(℃):155。

毒理学数据:

急性毒性LD50雄、雌小鼠,雄、雌大鼠(mg/kg):143,193,1982,1459口服.急性毒性LD50雄、雌小鼠(mg/kg):7.3,9.1腹腔注射.

CHEMICAL IDENTIFICATION

RTECS NUMBER :
US7975620
CHEMICAL NAME :
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2- oxopropyl ester
CAS REGISTRY NUMBER :
86780-90-7
LAST UPDATED :
199612
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C19-H22-N2-O7
MOLECULAR WEIGHT :
390.43

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 :
1459 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Blood - normocytic anemia Nutritional and Gross Metabolic - body temperature decrease
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: 21(Suppl 4),S931,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
143 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Blood - normocytic anemia
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: 21(Suppl 4),S931,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
7300 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Blood - normocytic anemia
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: 21(Suppl 4),S931,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
3333 mg/kg
TOXIC EFFECTS :
Cardiac - change in rate Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
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: 21(Suppl 4),S931,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1365 mg/kg/13W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in spleen
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: 21(Suppl 4),S947,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3650 mg/kg/1Y-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Kidney, Ureter, Bladder - urine volume increased Blood - changes in erythrocyte (RBC) count
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: 21(Suppl 4),S1013,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
6825 mg/kg/13W-I
TOXIC EFFECTS :
Blood - change in clotting factors Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - 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: 21(Suppl 4),S977,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
18200 mg/kg/52W-I
TOXIC EFFECTS :
Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate Blood - pigmented or nucleated red blood cells
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: 21(Suppl 4),S1041,1993 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
165 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) 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: 21(Suppl 4),S1095,1993
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 - viability index (e.g., # alive at day 4 per # born alive)
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: 21(Suppl 4),S1139,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
468 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - behavioral
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: 21(Suppl 4),S1139,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
500 mg/kg
SEX/DURATION :
female 6-15 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 - 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: 21(Suppl 4),S1115,1993

化合物(I)和3-氨基丁烯酸[2,2-(亚乙基二氧基)丙基]酯在乙醇中回流,缩合环合得到化合物(Ⅱ),再酸性水解得到产物。