30484-77-6

• 常用中文名：盐酸氟桂利嗪
• 常用英文名：Flunarizine 2HCl
• CAS号：30484-77-6
• 分子式：C₂₆H₂₈Cl₂F₂N₂
• 分子量：477.417
• 相关类别： 原料药 循环系统用药 周围血管扩张药
• 发布时间：2018-05-23 08:00:00
• 更新时间：2024-01-05 17:27:34
• Flunarizine是钙离子通道阻断剂。
• 盐酸氟桂利嗪是一种钙通道阻断剂。能防止因缺血等原因导致的细胞内病理性钙超载而造成的细胞损害。盐酸氟桂利嗪具有：
  （1）缓解血管痉挛，对血管收缩物质引起的持续性血管痉挛有持久的抑制作用，尤其对基底动脉和颈内动脉明显，其作用比脑益嗪强15倍；
  （2）前庭抑制作用，能增加耳蜗小动脉血流量，改善前庭器官循环；
  （3）抗癫痫作用，可阻断神经细胞的病理性钙超载而防止阵发性去极化，细胞放电，从而避免癫痫发作；
  （4）保护心肌，明显减轻缺血性心肌损害；
  （5） 氟桂利嗪尚有改善肾功能之作用，可用于慢性肾功能衰竭；另外盐酸氟桂利嗪还有抗组织胺作用。

名称

• 中文名: 盐酸氟桂利嗪
• 英文名: Flunarizine Dihydrochloride
• 中文别名: (E)-1-[双(4-氟苯基)甲基]-4-(3-苯基-2-丙烯基)-哌嗪二盐酸盐; 盐酸氟桂嗪
• 英文别名: Gradient; Mondus; Sibelium; Fluxarten; Issium; Flugeral; Piperazine, 1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenyl-2-propen-1-yl]-, hydrochloride (1:2); Flunarizine dihydrochloride; EINECS 250-216-6; 1-[Bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine dihydrochloride; 1-(Bis(4-fluorophenyl)methyl)-4-cinnamylpiperazine dihydrochloride; 1-[Bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenyl-2-propen-1-yl]piperazine dihydrochloride; Flunagen; Dinaplex; MFCD00058198; Flunarizine 2HCl; Flunarl; Flunarizine HCl; Flunarizine (dihydrochloride)

物化性质

• 沸点: 511.3ºC at 760 mmHg
• 熔点: 204-210ºC
• 分子式: C₂₆H₂₈Cl₂F₂N₂
• 分子量: 477.417
• 闪点: 263ºC
• 精确质量: 476.159760
• PSA: 6.48000
• LogP: 6.86500
• 外观性状: 白色结晶粉末,无气味的
• 储存条件:

  密封、在2 ºC -8 ºC下保存

• 稳定性:

  如果遵照规格使用和储存则不会分解，未有已知危险反应

• 水溶解性: chloroform/methanol (9:1): 50 mg/mL, clear, colorless
• 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:4

  4.可旋转化学键数量:6

  5.互变异构体数量:无

  6.拓扑分子极性表面积6.5

  7.重原子数量:32

  8.表面电荷:0

  9.复杂度:487

  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:0

  13.确定化学键立构中心数量:1

  14.不确定化学键立构中心数量:0

  15.共价键单元数量:3

• 更多:

  1. 性状：未确定

  2. 密度（g/mL,20℃）：未确定

  3. 相对蒸汽密度（g/mL,空气=1）：未确定

  4. 熔点（ºC）：未确定

  5. 沸点（ºC,常压）：未确定

  6. 沸点（ºC,KPa）：未确定

  7. 折射率：未确定

  8. 闪点（ºC）：未确定

  9. 比旋光度（º）：未确定

  10. 自燃点或引燃温度（ºC）：未确定

  11. 蒸气压（Pa,20ºC）：未确定

  12. 饱和蒸气压（KPa,25ºC）：未确定

  13. 燃烧热（KJ/mol）：未确定

  14. 临界温度（ºC）：未确定

  15. 临界压力（KPa）：未确定

  16. 油水（辛醇/水）分配系数的对数值：未确定

  17. 爆炸上限（%,V/V）：未确定

  18. 爆炸下限（%,V/V）：未确定

  19. 溶解性：溶于氯仿：甲醇=9：1，50mg/mL

生物活性

• 描述: Flunarizine是钙离子通道阻断剂。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钙通道
  研究领域 >> 神经疾病
• 参考文献:

  [1]. http://en.wikipedia.org/wiki/Flunarizine

MSDS

Section 1. Chemical Product and Company Identification Flunarizine Dihydrochloride Common Name/ Trade Name Flunarizine Dihydrochloride Section 4. First Aid Measures Eye ContactCheck for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at least 15 minutes. Get medical attention if irritation occurs. Skin ContactWash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops. Serious Skin ContactNot available. InhalationIf inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical attention. Serious InhalationNot available. IngestionDo NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen tight clothing such as a collar, tie, belt or waistband. Serious IngestionNot available. Section 5. Fire and Explosion Data Flammability of the Product May be combustible at high temperature. Auto-Ignition Temperature Not available. Flash PointsNot available. Flammable LimitsNot available. Products of CombustionThese products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), halogenated compounds. Fire Hazards in Presence of Slightly flammable to flammable in presence of heat. Various Substances Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available. Risks of explosion of the product in presence of static discharge: Not available. of Various Substances SMALL FIRE: Use DRY chemical powder. Fire Fighting Media and InstructionsLARGE FIRE: Use water spray, fog or foam. Do not use water jet. As with most organic solids, fire is possible at elevated temperatures Material in powder form, capable of creating Special Remarks on a dust explosion. Fire Hazards Special Remarks on Explosion Not available. Hazards Section 6. Accidental Release Measures Small SpillUse appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by spreading water on the contaminated surface and dispose of according to local and regional authority requirements. Large SpillUse a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water on the contaminated surface and allow to evacuate through the sanitary system. Flunarizine Dihydrochloride Section 7. Handling and Storage PrecautionsKeep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not ingest. Do not breathe dust. Wear suitable protective clothing. If ingested, seek medical advice immediately and show the container or the label. StorageKeep container tightly closed. Keep container in a cool, well-ventilated area. Do not store above 8°C(46.4°F). Refrigerate Section 8. Exposure Controls/Personal Protection Engineering ControlsUse process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to airborne contaminants below the exposure limit. Personal ProtectionSafety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves. Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used a Large Spillto avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist BEFORE handling this product. Exposure LimitsNot available. Section 9. Physical and Chemical Properties Physical state and appearance Solid. (Powdered solid.)OdorNot available. TasteNot available. Molecular Weight477.42 g/mole ColorWhite. pH (1% soln/water)Not available. Not available. Boiling Point Melting PointNot available. Not available. Critical Temperature Specific GravityNot available. Vapor PressureNot applicable. Vapor DensityNot available. VolatilityNot available. Odor ThresholdNot available. Water/Oil Dist. Coeff.Not available. Ionicity (in Water)Not available. Dispersion PropertiesNot available. SolubilitySolubility in CHCl3/Methanol (1:1): 50 mg/ml Section 10. Stability and Reactivity Data The product is stable. Stability Instability TemperatureNot available. Conditions of InstabilityExcess heat, dust generation Not available. Incompatibility with various substances Not available. Corrosivity Flunarizine Dihydrochloride Not available. Special Remarks on Reactivity Not available. Special Remarks on Corrosivity PolymerizationWill not occur. Section 11. Toxicological Information Routes of EntryInhalation. Ingestion. Toxicity to AnimalsAcute oral toxicity (LD50): 285 mg/kg [Mouse]. Chronic Effects on Humans Not available. Other Toxic Effects onSlightly hazardous in case of skin contact (irritant), of ingestion, of inhalation. Humans Special Remarks on Not available. Toxicity to Animals Special Remarks onMay cause adverse reproductive effects and birth defects (teratogenic) based on animal test data. Chronic Effects on Humans Special Remarks on otherAcute Potential Health Effects:\ Toxic Effects on HumansSkin: May cause skin irritation. Eyes: Dust may cause eye irritation. Inhalation: Inhalation of dust (poweder) may cause respiratory tract irritation. Ingestion: May be harmful if swallowed. May cause nausea, vomiting. May affect behavior/central nervous system (ataxia, somnolence, convulsions), respiration (dyspnea, cyanosis), eyes (ptosis), hair/skin. Chronic Potential Health Effects: Ingestion: Prolonged or repeated ingestion may cause nausea, vomiting, weight loss, convulsions. Section 12. Ecological Information EcotoxicityNot available. BOD5 and CODNot available. Products of BiodegradationPossibly hazardous short term degradation products are not likely. However, long term degradation products may arise. Toxicity of the ProductsThe products of degradation are as toxic as the product itself. of Biodegradation Special Remarks on theNot available. Products of Biodegradation Section 13. Disposal Considerations Waste DisposalWaste must be disposed of in accordance with federal, state and local environmental control regulations. Section 14. Transport Information DOT ClassificationNot a DOT controlled material (United States). IdentificationNot applicable. Not applicable. Special Provisions for Transport Flunarizine Dihydrochloride DOT (Pictograms) Section 15. Other Regulatory Information and Pictograms No products were found. Federal and State Regulations CaliforniaCalifornia prop. 65: This product contains the following ingredients for which the State of California has found to cause cancer which would require a warning under the statute: No products were found. Proposition 65 Warnings California prop. 65: This product contains the following ingredients for which the State of California has found to cause birth defects which would require a warning under the statute: No products were found. Other RegulationsOSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200). EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances (EINECS No. 250-216-6). Canada: Not listed on Canadian Domestic Substance List (DSL) or Canadian Non-Domestic Substances List (NDSL) China: Not listed on National Inventory. Japan: Not listed on National Inventory (ENCS). Korea: Not listed on National Inventory (KECI). Philippines: Not listed on National Inventory (PICCS). Australia: Listed on AICS. Other ClassificationsWHMIS (Canada) Not controlled under WHMIS (Canada). DSCL (EEC)R22- Harmful if swallowed.S46- If swallowed, seek medical advice immediately and show this container or label. Health Hazard HMIS (U.S.A.)1 National Fire Protection 1 Flammability 1 Association (U.S.A.) Fire Hazard 1 0 Reactivity Health Reactivity 0 Specific hazard Personal Protection E WHMIS (Canada) (Pictograms) DSCL (Europe) (Pictograms) TDG (Canada) (Pictograms) ADR (Europe) (Pictograms) Protective Equipment Gloves. Flunarizine Dihydrochloride Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. SECTION 16 - ADDITIONAL INFORMATION N/A

毒性和生态

生态学数据: 若无政府许可，勿将材料排入周围环境。 CHEMICAL IDENTIFICATION RTECS NUMBER : TK9187000 CHEMICAL NAME : Piperazine, 1-(bis(p-fluorophenyl)methyl)-4-cinnamyl-, dihydrochloride, (E)- CAS REGISTRY NUMBER : 30484-77-6 LAST UPDATED : 199609 DATA ITEMS CITED : 16 MOLECULAR FORMULA : C26-H26-F2-N2.2Cl-H MOLECULAR WEIGHT : 477.46 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 : 503 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - ptosis 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: 25,1408,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 305 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - ataxia 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: 16,1735,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1793 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - ataxia Skin and Appendages - hair 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: 16,1735,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 35 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis 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: 16,1735,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 285 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0187639 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 379 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis 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: 16,1735,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >2550 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - ataxia Skin and Appendages - hair 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: 16,1735,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 27 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis 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: 16,1735,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting 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: 16,1735,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 12720 mg/kg/26W-I TOXIC EFFECTS : Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death 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: 16,1783,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2400 mg/kg/30D-C TOXIC EFFECTS : Related to Chronic Data - death 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: 16,1748,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 7200 mg/kg/90D-C TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting Related to Chronic Data - death 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: 16,1809,1982 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 330 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) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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: 16,1840,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 33 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - physical 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: 16,1840,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 120 mg/kg SEX/DURATION : female 18-21 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) 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: 16,1860,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 286 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetal death 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: 16,1840,1982

安全

• 符号: GHS07
• 信号词: Warning
• 危害声明: H302
• 警示性声明: P301 + P312 + P330
• 个人防护装备: dust mask type N95 (US);Eyeshields;Gloves
• 危害码 (欧洲): Xn:Harmful;
• 风险声明 (欧洲): R22
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 3
• RTECS号: TK9187000
• 海关编码: 2933599090

海关

海关编码	2933599090
中文概述	2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 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:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%