161804-20-2

• 常用中文名：苯扎米尔盐酸盐
• 常用英文名：Benzamil
• CAS号：161804-20-2
• 分子式：C₁₃H₁₅Cl₂N₇O
• 分子量：356.21
• 相关类别： 信号通路 跨膜转运 钠通道
• 发布时间：2016-11-30 05:10:17
• 更新时间：2024-01-03 19:11:49
• Benzamil hydrochloride 是钠通道(ENaC)的特异性阻断剂。

名称

• 中文名: 苯扎米尔盐酸盐
• 英文名: 3,5-diamino-N-(N'-benzylcarbamimidoyl)-6-chloropyrazine-2-carboxamide,hydrochloride
• 英文别名: Prestwick_985; Benzylamiloride hydrochloride; Benzamil hydrochloride; Benzamil HCl; Benzamil hydrochloride hydrate; N-(Benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride hydrate

物化性质

• 分子式: C₁₃H₁₅Cl₂N₇O
• 分子量: 356.21
• PSA: 43.09000
• LogP: 2.28780
• 储存条件: 2-8℃

生物活性

• 描述: Benzamil hydrochloride 是钠通道(ENaC)的特异性阻断剂。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 心血管疾病
  研究领域 >> 代谢疾病
• 靶点:

  Sodium channel[1]

• 体外研究: 特异性ENaC阻断剂苯扎米尔盐酸盐加入管腔灌注液(10-6 M)显着降低基线[Na +] i 19.2 mM(n = 5),几乎完全抑制[Na +] i的[NaCl] L依赖性增加与腔内AngII合作[2]。
• 体内研究: 侧脑室注射盐酸苯甲酰胺载体后,脑室内注射内皮素-1(1nmol)显着增加平均动脉压和腹部交感神经活动10分钟。在SHRSP中,1或10 nmol/kg /天盐酸苯扎米尔的脑室内输注降低收缩压(第4天：F = 6.131,1 nmol/kg /天,P <0.05,10 nmol/kg /天,P <0.01第5天：F = 6.842,1nmol/kg /天,P <0.05,10nmol/kg /天,P <0.01;第6天：F = 5.988,1nmol/kg /天,P <0.05,10nmol/kg /天,P <0.01;第7天：F = 7.935,1nmol/kg /天,P <0.01,10nmol/kg /天,P <0.01),血管加压素的尿排泄(第5天：F = 9.385) ,1 nmol/kg /天,P <0.05,10 nmol/kg /天,P <0.05;第6天：F = 8.783,1 nmol/kg /天,P <0.01,10 nmol/kg /天,P < 0.01;第7天：F = 8.996,1nmol/kg /天,P <0.01,10nmol/kg /天,P <0.01)和去甲肾上腺素(第3天：F = 4.341,1nmol/kg /天,P <0.05,10nmol/kg /天,P <0.01;第4天：F = 9.865,1nmol/kg /天,P <0.01,10nmol/kg /天,P <0.01;第5天：F = 14.652, 1 nmol/kg/day,P <0.01,10 nmol/kg/day,P <0.01;第6天：F = 13.376,1 nmol/kg/day,P <0.01,10 nmol/kg/day,P <0.01第7天：与载体[1]相比,F = 8.594,1nmol/kg /天,P <0.01,10nmol/kg /天,P <0.01)。
• 细胞实验: 从兔和小鼠肾切割出单独的CCD片段。[Na +] i的测量值用作Na +跨顶膜转运的反映。通过施用10-6M的ENaC阻断剂苯扎米尔盐酸盐（一种不影响Na +：H +交换的浓度）来评估EnaC特异性活性。实验在存在/不存在管腔苯扎米尔盐酸盐或Na：H交换阻断剂HOE694的情况下进行，有/无AT1受体阻断剂坎地沙坦。最终的DMSO浓度低于0.1％[2]。
• 动物实验: 用于麻醉大鼠的急性脑室内注射。将引导插管插入右侧脑室，盐酸苯甲酰胺（0.1nmol / kg，n = 6; 1nmol / kg，n = 6; 10nmol / kg，n = 7）或载体（n = 6）在开始脑室内输注高渗NaCl之前15分钟，通过连接到微量注射器的套管将右侧脑室注入右侧脑室。每次注射包括10μL的体积，在30秒的时间内手动递送。为了研究盐酸苯甲酰胺对侧脑室注射除高渗NaCl之外的加压剂引起的升压反应的影响，脑内注射（1 nmol /10μL）脑内注射具有强效升压作用的内皮素-1脑室内注射苯扎米尔盐酸盐（10nmol / kg，n = 6）或载体（n = 6）后15分钟，记录平均动脉压，心率和腹部交感神经发作20分钟。将导管植入用尿道麻醉的12周龄雄性大鼠的股动脉和静脉中。两个导管都填充有肝素化盐水（50U / mL）。在开始脑室内输注高渗NaCl前15分钟，将苯扎米尔盐酸盐（10nmol / kg，n = 6）或载体（10μL，n = 6）注入通过直接插入微量注射器连接到股静脉导管的管中，通过导管注入0.1ml等渗盐溶液，将内容物输送到静脉循环中[1]。
• 参考文献:

  [1]. Nishimura M, et al. Benzamil blockade of brain Na+ channels averts Na(+)-induced hypertension in rats. Am J Physiol. 1998 Mar;274(3 Pt 2):R635-44.

  [2]. Peti-Peterdi J, et al. Angiotensin II directly stimulates ENaC activity in the cortical collecting duct via AT(1) receptors. J Am Soc Nephrol. 2002 May;13(5):1131-5.

MSDS

Section1. IDENTIFICATION OF THE SUBSTANCE/MIXTURE Product identifiers Product name: Benzamil hydrochloride hydrate CAS-No.: 161804-20-2 Relevant identified uses of the substance or mixture and uses advised against Identified uses: Laboratory chemicals, Manufacture of substances Section2. HAZARDS IDENTIFICATION Classification of the substance or mixture Classification according to Regulation (EC) No 1272/2008 [EU-GHS/CLP] Skin irritation (Category 2) Eye irritation (Category 2) Specific target organ toxicity - single exposure (Category 3) Classification according to EU Directives 67/548/EEC or 1999/45/EC Irritating to eyes, respiratory system and skin. Label elements Labelling according Regulation (EC) No 1272/2008 [CLP] Pictogram Signal wordWarning Hazard statement(s) H315Causes skin irritation. H319Causes serious eye irritation. H335May cause respiratory irritation. Precautionary statement(s) P261Avoid breathing dust/ fume/ gas/ mist/ vapours/ spray. P305 + P351 + P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. Supplemental Hazardnone Statements Safety data sheet available on request. According to European Directive 67/548/EEC as amended. Hazard symbol(s) R-phrase(s) R36/37/38Irritating to eyes, respiratory system and skin. S-phrase(s) S26In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36Wear suitable protective clothing. Other hazards - none Section3. COMPOSITION/INFORMATION ON INGREDIENTS Substances Synonyms: N-(Benzylamidino)-3,5-diamino-6- chloropyrazinecarboxamidehydrochloridehydrate Formula: C13H14ClN7O · HCl · xH2O Molecular Weight: 356,21 g/mol ComponentConcentration Benzamil hydrochloride CAS-No.161804-20-2- Section4. FIRST AID MEASURES Description of first aid measures General advice Consult a physician. Show this safety data sheet to the doctor in attendance. If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician. In case of skin contact Wash off with soap and plenty of water. Consult a physician. In case of eye contact Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician. Most important symptoms and effects, both acute and delayed To the best of our knowledge, the chemical, physical, and toxicological properties have not been thoroughly investigated. Indication of any immediate medical attention and special treatment needed no data available Section5. FIREFIGHTING MEASURES Extinguishing media Suitable extinguishing media Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Special hazards arising from the substance or mixture Carbon oxides, nitrogen oxides (NOx), Hydrogen chloride gas Advice for firefighters Wear self contained breathing apparatus for fire fighting if necessary. Further information no data available Section6. ACCIDENTAL RELEASE MEASURES Personal precautions, protective equipment and emergency procedures Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. Environmental precautions Do not let product enter drains. Methods and materials for containment and cleaning up Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed containers for disposal. Reference to other sections For disposal see section 13. Section7. HANDLING AND STORAGE Precautions for safe handling Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed. Conditions for safe storage, including any incompatibilities Store in cool place. Keep container tightly closed in a dry and well-ventilated place. Recommended storage temperature: 2 - 8 °C Specific end uses no data available Section8. EXPOSURE CONTROLS/PERSONAL PROTECTION Control parameters Components with workplace control parameters Exposure controls Appropriate engineering controls Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. Personal protective equipment Eye/face protection Safety glasses with side-shields conforming to EN166 Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin protection Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. Body Protection impervious clothing, The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Respiratory protection For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). Section9. PHYSICAL AND CHEMICAL PROPERTIES Information on basic physical and chemical properties a) AppearanceForm: solid b) Odourno data available c) Odour Thresholdno data available d) pHno data available e) Melting point/freezingno data available point f) Initial boiling point and no data available boiling range g) Flash pointno data available h) Evaporation rateno data available i) Flammability (solid, gas) no data available j) Upper/lowerno data available flammability or explosive limits k) Vapour pressureno data available l) Vapour densityno data available m) Relative densityno data available n) Water solubilityno data available o) Partition coefficient: n- no data available octanol/water p) Autoignitionno data available temperature q) Decompositionno data available temperature r) Viscosityno data available s) Explosive propertiesno data available t) Oxidizing propertiesno data available Other safety information no data available Section10. STABILITY AND REACTIVITY Reactivity no data available Chemical stability no data available Possibility of hazardous reactions no data available Conditions to avoid no data available Incompatible materials Strong oxidizing agents Hazardous decomposition products Other decomposition products - no data available Section11. TOXICOLOGICAL INFORMATION Information on toxicological effects Acute toxicity no data available Skin corrosion/irritation no data available Serious eye damage/eye irritation no data available Respiratory or skin sensitization no data available Germ cell mutagenicity no data available Carcinogenicity IARC:No component of this product present at levels greater than or equal to 0.1% is identified as probable, possible or confirmed human carcinogen by IARC. Reproductive toxicity no data available Specific target organ toxicity - single exposure Inhalation - May cause respiratory irritation. Specific target organ toxicity - repeated exposure no data available Aspiration hazard no data available Potential health effects InhalationMay be harmful if inhaled. Causes respiratory tract irritation. IngestionMay be harmful if swallowed. SkinMay be harmful if absorbed through skin. Causes skin irritation. EyesCauses serious eye irritation. Signs and Symptoms of Exposure To the best of our knowledge, the chemical, physical, and toxicological properties have not been thoroughly investigated. Additional Information RTECS: Not available Section12. ECOLOGICAL INFORMATION Toxicity no data available Persistence and degradability no data available Bioaccumulative potential no data available Mobility in soil no data available Results of PBT and vPvB assessment no data available Other adverse effects no data available Section13. DISPOSAL CONSIDERATIONS Waste treatment methods Product Offer surplus and non-recyclable solutions to a licensed disposal company. Dissolve or mix the material with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber. Contaminated packaging Dispose of as unused product. Section14. TRANSPORT INFORMATION UN number ADR/RID: -IMDG: -IATA: - UN proper shipping name ADR/RID: Not dangerous goods IMDG: Not dangerous goods IATA:Not dangerous goods Transport hazard class(es) ADR/RID: -IMDG: -IATA: - Packaging group ADR/RID: -IMDG: -IATA: - Environmental hazards ADR/RID: noIMDG Marine pollutant: noIATA: no Special precautions for user no data available Section15. REGULATORY INFORMATION This safety datasheet complies with the requirements of Regulation (EC) No. 1907/2006. Safety, health and environmental regulations/legislation specific for the substance or mixture no data available Chemical Safety Assessment no data available Section16. OTHER INFORMATION Further information Copyright 2012 Co. LLC. License granted to make unlimited paper copies for internal use only. The above information is believed to be correct but does not purport to be all inclusive and shall be used only as a guide. The information in this document is based on the present state of our knowledge and is applicable to the product with regard to appropriate safety precautions. It does not represent any guarantee of the properties of the product. Corporation and its Affiliates shall not be held liable for any damage resulting from handling or from contact with the above product. See and/or the reverse side of invoice or packing slip for additional terms and conditions of sale.

安全

• 危害码 (欧洲): Xi
• 风险声明 (欧洲): R36/37/38
• 安全声明 (欧洲): S26
• 海关编码: 2924299090

海关

海关编码	2924299090
中文概述	2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%
申报要素	品名, 成分含量, 用途, 包装
Summary	2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%