6138-79-0

• 常用中文名：盐酸曲普利啶
• 常用英文名：Triprolidine hydrochloride
• CAS号：6138-79-0
• 分子式：C₁₉H₂₅ClN₂O
• 分子量：314.85200
• 相关类别： 原料药 抗变态反应药 抗组胺药
• 发布时间：2018-04-07 08:00:00
• 更新时间：2024-01-02 20:34:59
• 盐酸曲普利啶是一种口服活性、细胞渗透性和第一代组胺H1拮抗剂[1]。盐酸曲普利啶是一种抗组胺药,可用于过敏性鼻炎、哮喘和荨麻疹[2]。

名称

• 中文名: 盐酸曲普利啶
• 英文名: triprolidine hydrochloride monohydrate
• 英文别名: MFCD00150574; Triprolidine hydrochloride

物化性质

• 沸点: 462ºC at 760 mmHg
• 熔点: 115-120ºC
• 分子式: C₁₉H₂₅ClN₂O
• 分子量: 314.85200
• 闪点: 233.2ºC
• 精确质量: 314.15500
• PSA: 16.13000
• LogP: 4.65740
• 外观性状: 白色结晶粉末
• 储存条件: 2-8°C
• 稳定性: Stable, but discolours in light. Incompatible with strong oxidizing agents.
• 水溶解性: >=10 g/100 mL at 20 ºC

生物活性

• 描述: 盐酸曲普利啶是一种口服活性、细胞渗透性和第一代组胺H1拮抗剂[1]。盐酸曲普利啶是一种抗组胺药,可用于过敏性鼻炎、哮喘和荨麻疹[2]。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 靶点:

  H1 Receptor

• 体内研究: 曲普利啶(间隔内注射；0.5μl中0.5μM；破伤风后30、60和180 min)对基线fEPSPs没有显著影响,但是,与盐水注射(60 min时为208%)相比,步行时诱导的长时程增强(LTP)较小(60 min时为基线值的173%)[2]。动物模型：成年雄性Long-Evans TMN(tuberomamillary nucleus,TMN)损伤大鼠[2]剂量：0.5μl给药0.5μm：间隔内灌注；破伤风后30、60、180min结果：LTP的步行相关增强减弱。
• 参考文献:

  [1]. Tao Luo, et al. Endogenous Histamine Facilitates Long-Term Potentiation in the Hippocampus During WalkingJ Neurosci. 2010 Jun 9;30(23):7845-52.

  [2]. Sang-Chul Shin, et al. Controlled Release of Triprolidine Using Ethylene-Vinyl Acetate Membrane and Matrix Systems. Eur J Pharm Biopharm

MSDS

Section 1. Chemical Product and Company Identification Triprolidine HClCatalog T2856, T1127 Common Name/ Number(s). Trade Name CAS#550-70-9 Manufacturer RTECSNot available. SPECTRUM CHEMICAL MFG. CORP. TSCATSCA 8(b) inventory: Triprolidine HCl Commercial Name(s)Not available. CI# Not available. Synonym2[1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]pyridine IN CASE OF EMERGENCY hydrochloride Chemical NameNot available. Not available.CALL (310) 516-8000 Chemical Family Chemical FormulaC19H22N2.HCl SPECTRUM CHEMICAL MFG. CORP. Section 2.Composition and Information on Ingredients Exposure Limits TWA (mg/m3)STEL (mg/m3) CEIL (mg/m3) NameCAS #% by Weight 1) Triprolidine HCl550-70-9100 Toxicological DataTriprolidine HCl: on IngredientsORAL (LD50):Acute: 840 mg/kg [Rat]. 495 mg/kg [Mouse]. Section 3. Hazards Identification Potential Acute Health Effects Hazardous in case of ingestion. Slightly hazardous in case of skin contact (irritant), of eye contact (irritant), of inhalation. Potential Chronic HealthHazardous in case of ingestion. EffectsSlightly hazardous in case of skin contact (irritant), of eye contact (irritant), of inhalation. CARCINOGENIC EFFECTS: Not available. MUTAGENIC EFFECTS: Not available. TERATOGENIC EFFECTS: Not available. DEVELOPMENTAL TOXICITY: Not available. Triprolidine HCl Section 4. First Aid Measures Eye ContactNo known effect on eye contact, rinse with water for a few minutes. Skin ContactAfter contact with skin, wash immediately with plenty of water. Gently and thoroughly wash the contaminated skin with running water and non-abrasive soap. Be particularly careful to clean folds, crevices, creases and groin. Cover the irritated skin with an emollient. If irritation persists, seek medical attention. Wash contaminated clothing before reusing. Serious Skin ContactNot available. InhalationAllow the victim to rest in a well ventilated area. Seek immediate medical attention. Serious InhalationNot available. IngestionDo not induce vomiting. Examine the lips and mouth to ascertain whether the tissues are damaged, a possible indication that the toxic material was ingested; the absence of such signs, however, is not conclusive. Loosen tight clothing such as a collar, tie, belt or waistband. If the victim is not breathing, perform mouth-to-mouth resuscitation. Seek immediate medical attention. 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...). Fire Hazards in Presence of Not available. Various Substances Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available. of Various SubstancesRisks of explosion of the product in presence of static discharge: Not available. Fire Fighting MediaSMALL FIRE: Use DRY chemical powder. and InstructionsLARGE FIRE: Use water spray, fog or foam. Do not use water jet. Special Remarks onNot available. 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. Triprolidine HCl Section 7. Handling and Storage PrecautionsKeep away from heat. Keep away from sources of ignition. Empty containers pose a fire risk, evaporate the residue under a fume hood. 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 dry. Keep in a cool place. Ground all equipment containing material. Keep container tightly closed. Keep in a cool, well-ventilated place. Combustible materials should be stored away from extreme heat and away from strong oxidizing agents. 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.OdorNot available. TasteNot available. 314.86 g/mole Molecular Weight ColorNot available. pH (1% soln/water)Not available. Boiling PointDecomposes. Melting Point115°C (239°F) Critical TemperatureNot available. Specific GravityNot available. Not applicable. Vapor Pressure Vapor DensityNot available. VolatilityNot available. Odor ThresholdNot available. Water/Oil Dist. Coeff.Not available. Not available. Ionicity (in Water) Dispersion PropertiesNot available. Not available. Solubility Section 10. Stability and Reactivity Data The product is stable. Stability Instability TemperatureNot available. Not available. Conditions of Instability Incompatibility with various Not available. substances Triprolidine HCl CorrosivityNon-corrosive in presence of glass. Special Remarks onNot available. Reactivity Special Remarks onNot available. Corrosivity PolymerizationNo. Section 11. Toxicological Information Routes of EntryIngestion. Toxicity to AnimalsAcute oral toxicity (LD50): 495 mg/kg [Mouse]. Chronic Effects on Humans Not available. Other Toxic Effects onHazardous in case of ingestion. HumansSlightly hazardous in case of skin contact (irritant), of inhalation. Special Remarks onNot available. Toxicity to Animals Special Remarks onNot available. Chronic Effects on Humans Special Remarks on otherNot available. Toxic Effects on Humans 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 less toxic than the product itself. of Biodegradation Special Remarks on theNot available. Products of Biodegradation Section 13. Disposal Considerations Waste Disposal Section 14. Transport Information DOT ClassificationNot a DOT controlled material (United States). IdentificationNot applicable. Special Provisions forNot applicable. Transport Triprolidine HCl DOT (Pictograms) Section 15. Other Regulatory Information and Pictograms TSCA 8(b) inventory: Triprolidine HCl 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). WHMIS (Canada) CLASS D-1B: Material causing immediate and serious toxic effects (TOXIC). Other Classifications DSCL (EEC)R22- Harmful if swallowed. Health Hazard HMIS (U.S.A.)2 National Fire Protection 1 Flammability 1 Association (U.S.A.) Fire Hazard 2 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. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Wear appropriate respirator when ventilation is inadequate. Triprolidine HCl SECTION 16 - ADDITIONAL INFORMATION N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UT7658000 CHEMICAL NAME : Pyridine, 2-(3-(1-pyrrolidinyl)-1-p-tolylpropenyl)-, monohydrochloride, monohydrate, stereoisomer CAS REGISTRY NUMBER : 6138-79-0 LAST UPDATED : 199803 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C19-H22-N2.Cl-H.H2-O MOLECULAR WEIGHT : 332.91 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 : 840 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 163 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 10760 mg/kg/90D-I TOXIC EFFECTS : Cardiac - changes in heart weight Gastrointestinal - changes in structure or function of salivary glands Blood - changes in leukocyte (WBC) count REFERENCE : JACTDZ Journal of the American College of Toxicology. (Mary Ann Liebert, Inc., 1651 Third Ave., New York, NY 10128) V.1-12, 1982-1993. Discontinued. Volume(issue)/page/year: 12,359,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 103 gm/kg/2Y-C TOXIC EFFECTS : Liver - changes in liver weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 27,223,1995 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 175 gm/kg/2Y-C TOXIC EFFECTS : Liver - other changes Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X2762 No. of Facilities: 269 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 4419 (estimated) No. of Female Employees: 2546 (estimated)

安全

• 符号: GHS07
• 信号词: Warning
• 危害声明: H302-H315-H319-H335
• 警示性声明: P301 + P312 + P330-P305 + P351 + P338
• 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;R36/37/38
• 安全声明 (欧洲): S26-S36
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 3
• RTECS号: UT7658000