59943-31-6

• 常用中文名：DU717
• 常用英文名：DU717
• CAS号：59943-31-6
• 分子式：C₁₂H₁₅ClN₄O₂S
• 分子量：314.79100
• 相关类别： 研究领域 心血管疾病
• 发布时间：2016-05-16 11:28:41
• 更新时间：2024-01-10 16:31:55
• DU-717 是一种抗高血压剂。

名称

• 中文名: DU717
• 英文名: 7-chloro-3-(4-methylpiperazin-1-yl)-4H-1λ6,2,4-benzothiadiazine 1,1-dioxide
• 英文别名: 2H-1,2,4-BENZOTHIADIAZINE,7-CHLORO-3-(4-METHYL-1-PIPERAZINYL)-,1,1-DIOXIDE; 1,1-Dioxyd 3-(4-methylpiperazinyl-1)-7-chlor-2H-1,2,4-benzthiadiazin; 7-Chloro-3-(4-methyl-1-piperazinyl)-4H-1,2,4-benzothiadiazine-1,1-dioxide; 7-Chloro-3-(4-methyl-1-piperazinyl)-2H-1,2,4-benzothiadiazine-1,1-dioxide; DU 717; DU717

物化性质

• 密度: 1.57g/cm3
• 沸点: 483.6ºC at 760 mmHg
• 分子式: C₁₂H₁₅ClN₄O₂S
• 分子量: 314.79100
• 闪点: 246.3ºC
• 精确质量: 314.06000
• PSA: 73.39000
• LogP: 1.58780
• 折射率: 1.712
• 储存条件: 库房低温,通风,干燥

生物活性

• 描述: DU-717 是一种抗高血压剂。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 心血管疾病
• 体内研究: 已经开发了一种气相色谱法,其能够准确测定血浆中新的抗高血压剂DU-717。在血浆中浓度范围为10至150 ng/mL的DU-717,相对标准偏差为6.2％时,可以进行准确的测定。最低可检测浓度为1 ng/mL。单次口服(10 mg/kg)后自发性高血压和正常血压大鼠血浆DU-717水平也已确定[1]。
• 动物实验: 大鼠[2] DU-717（100mg / kg每天，po）处理的SHRSP，SHRSP以HFC饮食（包括20％羊脂，5％胆固醇和2％胆酸）和1％NaCl在饮用水中饲喂， ALR和NAR，每组15只大鼠，用于EEG记录。将通过腹腔注射戊巴比妥（30mg / kg）麻醉的大鼠置于立体定位框架中以暴露颅骨，并且在两侧的额叶，顶叶和枕骨区域通过牙钻制造6个直径1mm的小孔。 。然后，将除了在尖端形成的小环以外的不锈钢电极（直径220μ）绝缘，以避免对硬脑膜和皮质的任何损伤，通过颅骨的孔插入并轻轻地固定在硬脑膜上。两侧的电极位于距中矢状线2mm处，并且额叶（F），顶骨（P），枕骨（O）电极分别位于耳间线前方5mm，2.5mm和0mm处。无差别电极（I）放置在前囟线上，前囟前4mm处。所有电极都用绝缘铜线连接到微型插座，整个组件嵌入牙科水泥中。手术后两周，脑电图重复记录数月。当记录脑电图时，大鼠处于透明的塑料笼（30×40×40cm）中并且可以自由移动。 EEG由ME-920记录，连接到自动分析仪MAF-5，光刺激器是MS-2PS。记录单极（IF，IP，IO）和双极（FP，PO，OF）。在清醒和困倦期间记录脑电图。记录校准为3厘米/秒和100μV/ 4毫米。
• 参考文献:

  [1]. Yamaguchi T, et al. Determination of 7-chloro-3-(4-methyl-1-piperazinyl)-4h-1,2,4-benzothiadiazine-1,1-dioxide (DU-717) in plasma using electron-capture gas chromatography. J Chromatogr. 1978 Oct 11;160(1):181-90.

  [2]. R Horie. rats (ALR) and normotensive atherogenic rats (NAR).

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DK8187000 CHEMICAL NAME : 2H-1,2,4-Benzothiadiazine, 7-chloro-3-(4-methyl-1-piperazinyl)-, 1,1-dioxide CAS REGISTRY NUMBER : 59943-31-6 LAST UPDATED : 199310 DATA ITEMS CITED : 8 MOLECULAR FORMULA : C12-H15-Cl-N4-O2-S MOLECULAR WEIGHT : 314.82 WISWESSER LINE NOTATION : T66 BSWN EMJ IG D- AT6N DNTJ D1 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 : >5 gm/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - tremor Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Behavioral - tremor Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 551 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - tremor Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >2412 mg/kg TOXIC EFFECTS : Behavioral - tremor Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 242 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 400 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - other changes REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 499 gm/kg/26W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - proteinuria Endocrine - changes in thymus weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,294,1980