7195-27-9

• 常用中文名：美夫西特
• 常用英文名：mefruside
• CAS号：7195-27-9
• 分子式：C₁₃H₁₉ClN₂O₅S₂
• 分子量：382.88300
• 相关类别： 原料药 泌尿系统用药 利尿药
• 发布时间：2018-08-20 10:42:49
• 更新时间：2024-01-05 17:22:27
• 美氟沙苷是一种口服活性利尿剂,具有轻微的降压作用。Mefruside抑制分离的大鼠肝脏灌注模型中尿素的合成。Mefruside可用于水肿和高血压的研究[1][2]。

名称

• 中文名: 美夫西特
• 英文名: 4-chloro-1-N-methyl-1-N-[(2-methyloxolan-2-yl)methyl]benzene-1,3-disulfonamide
• 中文别名: 甲呋速尿
• 英文别名: mefruside; FBA 1500; BAY 1500; Mefrusid; 1,3-Benzenedisulfonamide,4-chloro-N1-methyl-N1-((tetrahydro-2-methyl-2-furanyl)methyl); FDA 1902; Mefrusidum [INN-Latin]; Mefrusal; Baycaron; Mefrusida [INN-Spanish]

物化性质

• 密度: 1.417g/cm3
• 沸点: 565.2ºC at 760 mmHg
• 熔点: 149.5°C
• 分子式: C₁₃H₁₉ClN₂O₅S₂
• 分子量: 382.88300
• 闪点: 295.6ºC
• 精确质量: 382.04200
• PSA: 123.53000
• LogP: 4.03890
• 折射率: 1.571

生物活性

• 描述: 美氟沙苷是一种口服活性利尿剂,具有轻微的降压作用。Mefruside抑制分离的大鼠肝脏灌注模型中尿素的合成。Mefruside可用于水肿和高血压的研究[1][2]。
• 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: Mefruside(0.3 mM；50分钟)对离体灌注大鼠肝脏中尿素合成的抑制率为34%[1]。甲氟苷(0.25、0.5、0.75、1.25 mM)以浓度依赖性的方式抑制离体灌注大鼠肝脏中的尿素合成[1]。细胞活力测定[1]细胞系：大鼠肝脏(来自120-220g体重的雄性Wistar大鼠；分离的灌注模型)浓度：0.3mM孵育时间：50min结果：尿素合成的抑制率为34%。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CZ9195000 CHEMICAL NAME : m-Benzenedisulfonamide, 4-chloro-N(sup 1)-methyl-N(sup 1)-(tetrahydro-2-methylfurfuryl)- CAS REGISTRY NUMBER : 7195-27-9 LAST UPDATED : 199706 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C13-H19-Cl-N2-O5-S2 MOLECULAR WEIGHT : 382.91 WISWESSER LINE NOTATION : T5OTJ B1N1&SWR DG CSZW& B1 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 : >10 gm/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - chromodacryorrhea Nutritional and Gross Metabolic - body temperature decrease REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,1003,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9800 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - chromodacryorrhea Nutritional and Gross Metabolic - body temperature decrease REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,1003,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9800 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value 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: 6,386,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 500 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: 17,659,1967 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >10 gm/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Nutritional and Gross Metabolic - body temperature decrease REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,1003,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 5200 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Nutritional and Gross Metabolic - body temperature decrease REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,1003,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 5200 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value 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: 6,386,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 500 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: 17,659,1967 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - food intake (animal) Behavioral - ataxia REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,659,1967 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - cat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Behavioral - excitement Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,659,1967 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit 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: 17,659,1967 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 140 gm/kg/4W-C TOXIC EFFECTS : Liver - other changes Blood - other changes Nutritional and Gross Metabolic - changes in chlorine REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,1003,1973 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 52584 mg/kg/24W-I TOXIC EFFECTS : Behavioral - fluid intake Kidney, Ureter, Bladder - changes in both tubules and glomeruli Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,1019,1973