Indapamide 吲达帕胺

CAS 26807-65-8 MFCD00079375

化学结构图

26807-65-8
SMILES: CC1CC2C=CC=CC=2N1NC(=O)C1C=C(C(Cl)=CC=1)S(N)(=O)=O

化学属性

Mol. FormulaC16H16ClN3O3S
Mol. Weight365.86
Melting Point160-162°C

别名和识别编码

Chemical NameIndapamide
CAS Number26807-65-8
Synonym 茚磺苯酰胺 吲满胺 natrilix 3-(aminosulfonyl)-4-chloro-n-(2,3-dihydro-2-methyl-1h-indol-1-yl)-benzamid ipamix 吲达帕胺 4-chloro-n-(2-methyl-1-indolinyl)-3-sulfamoylbenzamide s1520 noranat N-(2-甲基-2,3-二氢-1H-吲哚基)-3-氨磺酰基-4-氯-苯甲酰胺 吲哒帕胺 3-(aminosulfonyl)-4-chloro-n-(2,3-dihydro-2-methyl-1h-indol-1-yl)benzamide tandix N-(4-CHLORO-3-SULFAMOYLBENZAMIDO)-2-METHYLINDOLINE 4-chloro-n-(2-methyl-1-indolinyl)-3-sulfamoyl-benzamid se-1520 indamol 吲满速尿 Benzamide, bajaten 吲达帕安 fludex Bajaten INDAPAMIDE indaflex 1-(4-chloro-3-sulfamoylbenzamido)-2-methylindoline damide 3-(Aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-1-yl)benzamide lozol N-[4-CHLORO-3-SULFAMOYL-BENZAMIDOL]-2-METHYLINDOLINE
MDL NumberMFCD00079375
PubChem Substance ID24895952
EC Number248-012-7
Chemical Name Translation吲达帕胺
Beilstein Registry Number1604026
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分类

  • Alphabetic, Analytical Standards, Analytical/Chromatography, Chemical Structure, Chromatography, Diuretic, Doping Substances, Drugs & Metabolites, Drugs of Abuse, Forensic and Veterinary Standards, I, Neat Compounds, Others
  • {SNA} All Doping Standards (A-Z), Alphabetic, Analytical Standards, Analytical/Chromatography, Chemical Structure, Chromatography, Diuretic, Doping Substances, Drugs & Metabolites, Drugs of Abuse, Forensic and Veterinary Standards, I,

产品应用

  • Used as an antihypertensive. Diuretic.

相关文献及参考

  • Leary, et al.: Curr. Ther. Res., 15, 571 (1973),
  • Kyncl, J., et al.: Arzneim.-Forsch., 25, 1491 (1975),
  • DiFeo, T.J., et al.: Anal. Profiles Drug Subs. Excip., 23, 229 (1994),
  • Merck 14 ,4935

安全信息

WGK Germany2
RTECSCV2451200 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - guinea pig
DOSE/DURATION           : 347 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 25,1491,1975

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - guinea pig
DOSE/DURATION           : >3 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year:

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >3 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 25,1491,1975

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - guinea pig
DOSE/DURATION           : 272 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 25,1491,1975

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 110 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)
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: 10,1337,1982

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 1100 mg/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   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: 10,1337,1982

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rabbit
DOSE                    : 260 mg/kg
SEX/DURATIO

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 270 mg/kg
SEX/DURATION            : female 17-22 day(s) after conception
                          lactating female 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
   Reproductive - Effects on Newborn - physical
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: 10,1363,1982

其他信息

  • MSDS 信息:N-(4-Chloro-3-sulfamoylbenzamido)-2-methylindoline(26807-65-8).msds
  • 储运特性:库房通风低温干燥
  • 急性毒性:口服-大鼠LD50: >;3000 毫克/公斤; 口服-小鼠LD50: >;3000 毫克/公斤
  • 毒性分级:中毒
  • MOL 文件:26807-65-8.mol
  • 灭火剂:干粉、泡沫、砂土、二氧化碳, 雾状水
  • 利尿降压药:白色针状结晶或结晶性粉末，无臭，无味。几乎不溶于水或稀盐酸，溶于乙醇或醋酸乙酯，易溶于丙酮、冰醋酸，微溶于氯仿或乙醚。 吲达帕胺是目前国内常用的一种非处方类利尿降压药，具有疗效好，降压平稳，副反应少等优点，最初由法国施维雅（Servier）制药公司首次研发开发，我国在1988年由天津力生制药首次成功开发了吲达帕胺薄膜衣片，商品名为“寿比山”。20世纪90年代中期，浙江普洛康裕制药、烟台西苑制药厂、浙江东日药业、东莞万成制药、山西亚宝药业、阜新芝田药业、濮阳汇元药业、重庆药友制药8家药厂获准生产制剂。90年代末，法国施维雅制药公司将吲达帕胺缓释片剂引入国内，商品名为“纳催离”。随后，吲达帕胺原料药国产化有了推进，目前国内有7家企业获准生产原料药品种。 吲达帕胺具有利尿和钙拮抗双重作用，通过抑制远曲小管近端的Na+重吸收，产生利尿作用，又阻滞Ca2+内流，对血管平滑肌有较高选择性，使外周小血管扩张，产生降压作用。但对血管平滑肌作用强于利尿作用，低于利尿剂量时即可降压，较高剂量时显示利尿作用，但无噻嗪类利尿药的缺点，即不引起体位性低血压、潮红和反射性心动过速，对血象、血脂、糖代谢及肾功能也无明显影响，治疗剂量对心率、心输出量、心电图均无明显改变，对中枢神经系统和植物神经无明显作用。口服2～3h产生降压效应，作用维持24h，单独用药效果良好。利尿作用3h出现，4～6h达最大效应。与其他利尿剂不同，本品脂溶性高，口服吸收后，在肝、肾血浆浓度最高，心、肺、肌肉、脂肪中浓度较低。本品主要以代谢产物和以5%的原型从肾脏排泄。吲达帕胺适用于轻、中度原发性高血压，亦可用于充血性心力衰竭引起的水钠潴留，对伴有肾衰、糖尿病、高血脂的高血压患者也适用，单用降压效果显著，与β受体阻滞剂合用疗效更佳，因为本药有利尿作用，可引起低血钾，可同时补充钾盐。
  • 可燃性危险特性:可燃;燃烧产生有毒氮氧化物, 硫氧化物和氯化物烟雾
  • 用途一:用于轻、中度原发性高血压。
  • Sigma Aldrich:26807-65-8(sigmaaldrich)
  • 类别:有毒物品

系列性分类

  1. Analytical & Chromatography 分析化学与色谱
  2. Analytical Standards
  3. Alphabetic - Analytical Standards
  4. I - Alphabetic
  1. Analytical & Chromatography 分析化学与色谱
  2. Analytical Standards
  3. Chromatography - Analytical Standards
  4. Forensic and Veterinary Standards - Chromatography
  5. Doping Substances - Forensic and Veterinary Standards
  6. Diuretic - Doping Substances

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