346-18-9

• 常用中文名：泊利噻嗪
• 常用英文名：polythiazide (200 mg)
• CAS号：346-18-9
• 分子式：C₁₁H₁₃ClF₃N₃O₄S₃
• 分子量：439.88200
• 相关类别： 原料药 泌尿系统用药 利尿药
• 发布时间：2018-06-07 20:34:32
• 更新时间：2024-01-14 13:48:41
• 聚噻嗪是一种有效的口服噻嗪利尿剂,具有抗高血压作用。聚噻嗪可减轻水肿,降低血压。聚噻嗪还具有光毒性[1][2][3]。

名称

• 中文名: 泊利噻嗪
• 英文名: 6-chloro-2-methyl-1,1-dioxo-3-(2,2,2-trifluoroethylsulfanylmethyl)-3,4-dihydro-1λ6,2,4-benzothiadiazine-7-sulfonamide
• 英文别名: Polythiazide; Polythiazidum; Politiazida; Nephril; P-2525; Renese; Drenusil

物化性质

• 密度: 1.598g/cm3
• 沸点: 580.1ºC at 760mmHg
• 熔点: 202.5°
• 分子式: C₁₁H₁₃ClF₃N₃O₄S₃
• 分子量: 439.88200
• 闪点: 304.7ºC
• 精确质量: 438.97100
• PSA: 151.63000
• LogP: 4.59280
• 折射率: 1.566
• 计算化学:

  1.疏水参数计算参考值（XlogP）:无

  2.氢键供体数量:2

  3.氢键受体数量:11

  4.可旋转化学键数量:4

  5.互变异构体数量:无

  6.拓扑分子极性表面积:152

  7.重原子数量:25

  8.表面电荷:0

  9.复杂度:692

  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

生物活性

• 描述: 聚噻嗪是一种有效的口服噻嗪利尿剂,具有抗高血压作用。聚噻嗪可减轻水肿,降低血压。聚噻嗪还具有光毒性[1][2][3]。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 其他 >> 其他
• 体外研究: 在蓝光2000装置(Ex:325nm)下,聚噻嗪(500μM,1分钟)诱导显著的光毒性NHIK 3025细胞死亡[2]。
• 体内研究: 聚噻嗪(口服灌胃,10 mg/kg,每日5天)增加了胆固醇喂养的C57BL/cdJ小鼠的血浆胆固醇水平[3]。多噻嗪(口服给药,0.4 mg/k g)对高血压狗和大鼠具有利尿和排尿作用[1]。动物模型：胆固醇喂养的C57BL/cdJ小鼠[3]剂量：10mg/kg给药：口服灌胃,每天5天结果：导致血浆总胆固醇水平上升约13%,非高密度脂蛋白分数增加。动物模型：高血压犬[1]剂量：0.4mg/kg给药：口服给药,每日5天结果：钠和氯的排泄增加。动物模型：高血压大鼠[1]剂量：0.05、0.1、0.2、0.4mg/kg给药：口服,每日两次,共3天。结果：显示利钠和利尿作用。
• 参考文献:

  [1]. A SCRIABINE, et al. Pharmacological studies with polythiazide, a new diuretic and antihypertensive agent. Proc Soc Exp Biol Med. 1961 Aug-Sep;107:864-72.

  [2]. E Selvaag, et al. Phototoxicity due to sulphonamide derived oral antidiabetics and diuretics: investigations in a cell culture model. Photodermatol Photoimmunol Photomed. 1996 Feb;12(1):1-6.

  [3]. M N Krupp, et al. Effects of doxazosin and other antihypertensives on serum lipid levels and lipoprotein lipase in the C57BR/cdJ mouse. J Cardiovasc Pharmacol. 1989;13 Suppl 2:S11-8; discussion S18-9.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DK9275000 CHEMICAL NAME : 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 6-chloro-3,4-dihydro-2-methyl- 3-(((2,2,2-trifluoroethyl)thio)methyl)-, 1,1-dioxide CAS REGISTRY NUMBER : 346-18-9 LAST UPDATED : 199709 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C11-H13-Cl-F3-N3-O4-S3 MOLECULAR WEIGHT : 439.90 WISWESSER LINE NOTATION : T66 BSWN EM DHJ C1 D1S1XFFF HG ISZW HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 300 ug/kg/5D-I TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - coma Nutritional and Gross Metabolic - other changes REFERENCE : AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 70,1163,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >10 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,775,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 400 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 29ZVAB "Handbook of Analytical Toxicology," Sunshine, I., ed., Cleveland, OH, Chemical Rubber Co., 1969 Volume(issue)/page/year: -,97,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,793,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,775,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 450 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 29ZVAB "Handbook of Analytical Toxicology," Sunshine, I., ed., Cleveland, OH, Chemical Rubber Co., 1969 Volume(issue)/page/year: -,97,1969