99522-79-9

• 常用中文名：普拉地平
• 常用英文名：Pranidipine
• CAS号：99522-79-9
• 分子式：C₂₅H₂₄N₂O₆
• 分子量：448.468
• 发布时间：2018-04-26 08:00:00
• 更新时间：2024-01-02 18:17:18
• Pranidipine (OPC-13340) 是一种高效且长效的 1,4-二氢吡啶钙通道 (calcium channel) 阻滞剂,具有抗高血压作用。

名称

• 中文名: 普拉地平
• 英文名: 3-O-methyl 5-O-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
• 英文别名: 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl (2E)-3-phenyl-2-propen-1-yl ester; methyl (2E)-3-phenylprop-2-en-1-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate; UNII:9DES9QVH58; Pranidipine; FRC 8411; (E)-Cinnamyl Methyl (±)-1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate; Methyl (2E)-3-phenyl-2-propen-1-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 618.9±55.0 °C at 760 mmHg
• 熔点: 140-142ºC
• 分子式: C₂₅H₂₄N₂O₆
• 分子量: 448.468
• 闪点: 328.1±31.5 °C
• 精确质量: 448.163422
• PSA: 110.45000
• LogP: 5.35
• 外观性状: 黄色固体
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.606
• 储存条件: 室温，干燥，密封

生物活性

• 描述: Pranidipine (OPC-13340) 是一种高效且长效的 1,4-二氢吡啶钙通道 (calcium channel) 阻滞剂,具有抗高血压作用。
• 靶点:

  Calcium channel[1]

• 参考文献:

  [1]. Nakayama N, et al. Antihypertensive activity of OPC-13340, a new potent and long-acting dihydropyridine calcium antagonist, in rats. J Cardiovasc Pharmacol. 1990 May;15(5):836-44.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : US7975680 CHEMICAL NAME : 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 3- phenyl-2-propenyl ester, (E)- CAS REGISTRY NUMBER : 99522-79-9 LAST UPDATED : 199703 DATA ITEMS CITED : 15 MOLECULAR FORMULA : C25-H24-N2-O6 MOLECULAR WEIGHT : 448.51 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 : 2968 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) 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: 21,1245,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 166 mg/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea 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: 21,1245,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1670 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - ptosis Skin and Appendages - dermatitis, other (after systemic exposure) 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: 21,1245,1993 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2551 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - ptosis 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: 21,1245,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 81 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation 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: 21,1245,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - ptosis 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: 21,1245,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >150 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4672068 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Gastrointestinal - nausea or vomiting 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: 21,1245,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2700 mg/kg/90D-I TOXIC EFFECTS : Cardiac - changes in heart weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - changes in chlorine 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: 21,1255,1993 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 : Blood - other changes Nutritional and Gross Metabolic - changes in calcium Related to Chronic Data - changes in uterine 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: 21,1327,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 2275 mg/kg/13W-I TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - urine volume increased Nutritional and Gross Metabolic - changes in chlorine 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: 21,1277,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 2190 mg/kg/1Y-I TOXIC EFFECTS : Cardiac - changes in heart weight Endocrine - changes in spleen 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: 21,1345,1993 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 8400 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 - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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: 21,1375,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 75 mg/kg SEX/DURATION : female 17-20 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - sex ratio 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: 21,1415,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 13 gm/kg SEX/DURATION : female 6-18 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) Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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: 21,1405,1993

安全

• 危害码 (欧洲): Xi