60560-33-0

• 常用中文名：吡那地尔
• 常用英文名：Pinacidil
• CAS号：60560-33-0
• 分子式：C₁₃H₁₉N₅
• 分子量：245.32300
• 相关类别： 原料药 循环系统用药 防治心绞痛药
• 发布时间：2018-07-26 11:10:33
• 更新时间：2024-01-07 19:17:46
• 吡那地尔是钾通道的有效激活剂。吡那地尔是一种抗高血压药物,通过开放K+通道使血管平滑肌超极化。吡那地尔显著改善再灌注功能和心脏顺应性。吡那地尔具有直接的心脏保护功效[1]。

名称

• 中文名: 吡那地尔
• 英文名: pinacidil
• 中文别名: (+/-)-N-氰基-N'-4-吡啶基-N''-(1,2,2-三甲基丙基)胍
• 英文别名: p1134; pinacidilmonohydrate; 2-cyano-3-(4-pyridyl)-1-(1,2,2-trimethylpropyl)guanidinemonohydrate; (+/-)-Pinacidil; 2-Cyano-3-(4-pyridyl)-1-(1,2,2-trimethylpropyl)guanidine; s-1230; 2-cyano-3-(4-pyridyl)-1-(1,2,2-trimethylpropyl)-guanidinmonohydrate; N"-cyano-N-4-pyridyl-N'-1,2,2,trimethyl propylguanidine; (+/-)-N-CYANO-N'-4-PYRIDINYL-N''-(1,2,2-TRIMETHYLPROPYL)GUANIDINE; Picacidil

物化性质

• 密度: 1.1402 (rough estimate)
• 沸点: 378.29°C (rough estimate)
• 熔点: 110-114℃
• 分子式: C₁₃H₁₉N₅
• 分子量: 245.32300
• 精确质量: 245.16400
• PSA: 73.10000
• LogP: 2.81868
• 外观性状: solid | white
• 折射率: 1.6500 (estimate)
• 水溶解性: ethanol: 14 mg/mL

生物活性

• 描述: 吡那地尔是钾通道的有效激活剂。吡那地尔是一种抗高血压药物,通过开放K+通道使血管平滑肌超极化。吡那地尔显著改善再灌注功能和心脏顺应性。吡那地尔具有直接的心脏保护功效[1]。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 靶点:

  potassium channel[1]

• 参考文献:

  [1]. Grover GJ, et al. Anti-ischemic effects of the potassium channel activators pinacidil and cromakalim and the reversal of these effects with the potassium channel blocker glyburide. J Pharmacol Exp Ther. 1989;251(1):98-104.

  [2]. Hamilton TC, et al. Cromakalim, nicorandil and pinacidil: novel drugs which open potassium channels in smooth muscle. Gen Pharmacol. 1989;20(1):1-9.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : MF0230000 CHEMICAL NAME : Guanidine, N-cyano-N'-4-pyridinyl-N''-(1,2,2-trimethylpropyl)-, monohydrate CAS REGISTRY NUMBER : 60560-33-0 LAST UPDATED : 199706 DATA ITEMS CITED : 11 MOLECULAR FORMULA : C13-H19-N5.H2-O MOLECULAR WEIGHT : 263.39 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 : 210 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,133,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 7070 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - acute pulmonary edema Blood - hemorrhage 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: 19,2473,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 155 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,133,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 412 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,133,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 177 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,133,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 5600 mg/kg/8W-I TOXIC EFFECTS : Cardiac - changes in heart weight Endocrine - changes in adrenal weight Related to Chronic Data - changes in ovarian weight REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,133,1985 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3276 mg/kg/26W-I TOXIC EFFECTS : Cardiac - changes in heart weight Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight REFERENCE : NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,133,1985 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 840 mg/kg SEX/DURATION : male 9 week(s) pre-mating female 2 week(s) pre-mating female 1-7 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 - Effects on Embryo or Fetus - fetal death 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: 19,2491,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 550 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 - 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: 19,2503,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 550 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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: 19,2503,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 650 mg/kg SEX/DURATION : female 17-21 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth) 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: 19,2531,1991

安全

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 22-36/37/38
• 安全声明 (欧洲): 36
• WGK德国: 3
• 海关编码: 2933399090

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%