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DU717

DU717用途

DU-717 是一种抗高血压剂。

DU717名称

[ CAS 号 ]:
59943-31-6

[ 中文名 ]:
DU717

[ 英文名 ]:
DU717

[英文别名 ]:

DU 717
DU717

DU717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).

[相关活性小分子]

DU717物理化学性质

[ 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

DU717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