乙酰唑胺钠
乙酰唑胺钠用途
碳酸酐酶抑制剂。利尿药。
乙酰唑胺钠名称
[ CAS 号 ]:
1424-27-7
[ 中文名 ]:
乙酰唑胺钠
[ 英文名 ]:
Acetazolamide
[英文别名 ]:
- Sodium acetazolamide
- Acetazolamide,Monosodium Salt
- Acetazolamide sodium
- Acetazolamide sodium salt
- UNII-429ZT169UH
乙酰唑胺钠生物活性
[ 描述 ]:
乙酰唑胺钠是乙酰唑酰胺的钠盐。乙酰唑胺是碳酸酐酶(CA)IX抑制剂,对hCA IX的IC50为30 nM。乙酰唑酰胺具有利尿、降压和抗淋菌活性[1][4][5][6]。
[ 相关类别 ]:
[体外研究]
乙酰唑胺也抑制hCA II,IC50为130 nM[1]。乙酰唑胺(Ace)是一种小的杂芳磺酰胺,以高亲和力结合各种碳酸酐酶,作为碳酸酐酶(CA)抑制剂[2]。与对照组相比,高乙酰唑胺浓度(AceH,50 nM)、顺铂(Cis;1µg/mL)和Cis联合低乙酰唑酰胺浓度(AceL,10 nM)治疗显著降低了Hep-2细胞的活力[2]。与对照组相比,乙酰唑胺/顺式联合治疗显著增加P53的表达水平,因为AceL+顺式和AceH+顺式治疗均导致P53蛋白表达水平显著增加。与对照组相比,Ace/Cis联合治疗显著降低bcl-2/bax表达率,并增加caspase-3蛋白的表达。与对照组相比,AceL、AceH、Cis和AceL+Cis治疗显著降低bcl-2/bax比率[2]。Ace和Cis联合治疗可有效促进Hep-2细胞凋亡[2]。Ace/Cis联合治疗可显著降低Hep-2细胞中AQP1 mRNA的表达。与对照组相比,AceH和AceL+Cis处理均降低了Hep-2细胞中水通道蛋白-1(AQP1)mRNA的表达[2]。
[体内研究]
乙酰唑胺(40 mg/kg)显著增强MS-275对神经母细胞瘤(NB)SH-SY5Y异种移植物肿瘤发生的抑制作用[3]。乙酰唑胺(40 mg/kg)和/或MS-275治疗可降低NB SH-SY5Y异种移植物中HIF1-α和CAIX的表达[3]。乙酰唑胺(40 mg/kg)、MS-275和乙酰唑酰胺+MS-275降低NB SH-SY5Y异种移植物中有丝分裂和增殖标记物的表达[3]。乙酰唑胺(50 mg/kg;PO,持续3天)显著降低感染小鼠阴道内淋菌负荷90%[6]。
[参考文献]
乙酰唑胺钠物理化学性质
[ 熔点 ]:
258-259ºC (EFFERVESCENCE)
[ 分子式 ]:
C4H5N4NaO3S2
[ 分子量 ]:
244.22700
[ 精确质量 ]:
243.97000
[ PSA ]:
142.87000
[ LogP ]:
0.78380
[ 外观性状 ]:
固体
[ 储存条件 ]:
库房通风低温干燥
乙酰唑胺钠毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- AC8400000
- CHEMICAL NAME :
- Acetamide, N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-, monosodium salt
- CAS REGISTRY NUMBER :
- 1424-27-7
- LAST UPDATED :
- 199609
- DATA ITEMS CITED :
- 20
- MOLECULAR FORMULA :
- C4-H5-N4-O3-S2.Na
- MOLECULAR WEIGHT :
- 244.24
- WISWESSER LINE NOTATION :
- T5NN DSJ CSZW EMV1 &-NA-
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >1 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 3 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 3 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 1500 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 1 gm/kg/10D-I
- TOXIC EFFECTS :
- Nutritional and Gross Metabolic - changes in sodium Nutritional and Gross Metabolic - changes in potassium
- REFERENCE :
- JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- DOSE :
- 1 gm/kg
- SEX/DURATION :
- female 10 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 1,51,1968
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1 gm/kg
- SEX/DURATION :
- female 10 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 1,51,1968
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 850 mg/kg
- SEX/DURATION :
- female 10 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 28,355,1983
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1 gm/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 10,221,1974
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 200 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 27,51,1983
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1 gm/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 28,45,1983
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 3 gm/kg
- SEX/DURATION :
- female 9-11 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetal death
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 28,45,1983
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 200 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 28,45,1983
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1500 mg/kg
- SEX/DURATION :
- female 13 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material)
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 15,199,1977
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1500 mg/kg
- SEX/DURATION :
- female 13 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 15,199,1977
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- DOSE :
- 300 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 4,95,1971
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- DOSE :
- 600 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - Central Nervous System
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 4,95,1971
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravaginal
- DOSE :
- 110 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 7,209,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5616 No. of Facilities: 17 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 223 (estimated) No. of Female Employees: 137 (estimated)
乙酰唑胺钠安全信息
[ 危害码 (欧洲) ]:
Xi
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