96-88-8

• 常用中文名：甲哌卡因
• 常用英文名：Mepivacaine
• CAS号：96-88-8
• 分子式：C₁₅H₂₂N₂O
• 分子量：246.34800
• 相关类别： 信号通路 跨膜转运 钠通道
• 发布时间：2019-02-17 18:28:08
• 更新时间：2024-01-06 12:43:40
• Mepivacaine 是一种酰胺型药剂,可暂时使局部失去知觉。Mepivacaine 与神经元细胞膜上特定的电压门控钠离子通道结合,抑制钠离子内流和膜去极化。

名称

• 中文名: 2-甲基-2,6-壬二烯-1-胺
• 英文名: mepivacaine
• 中文别名: N-(2,6-二甲基苯基)-1-甲基哌啶-2-羧酰胺
• 英文别名: N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide; N-(2,6-Dimethylphenyl)-1-methylpiperidine-2-carboxamide

物化性质

• 密度: 1.077 g/cm3
• 沸点: 383.062ºC at 760 mmHg
• 熔点: 150.5ºC
• 分子式: C₁₅H₂₂N₂O
• 分子量: 246.34800
• 闪点: 185.47ºC
• 精确质量: 246.17300
• PSA: 32.34000
• LogP: 2.73710
• 外观性状: 白色至黄色粉末或晶体
• 储存条件: 2-8°C

生物活性

• 描述: Mepivacaine 是一种酰胺型药剂,可暂时使局部失去知觉。Mepivacaine 与神经元细胞膜上特定的电压门控钠离子通道结合,抑制钠离子内流和膜去极化。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 神经疾病
• 体外研究: 甲哌卡因与神经元细胞膜上特定的电压门控钠离子通道结合,抑制钠离子内流和膜去极化。这会导致神经冲动的启动和传导受阻,并导致可逆的感觉丧失。与其他局麻药相比,该药起效快,作用时间适中[2]。甲哌卡因起效快(比普鲁卡因快),作用持续时间中等(比普鲁卡因短)[3]。甲哌卡因显示Na(v)1.8的优先使用依赖性块,S(-)-布比卡因显示TTXs Na(+)通道的首选项[4]。
• 参考文献:

  [1]. Froehle M, et al. ECMO for Cardiac Rescue after Accidental Intravenous Mepivacaine Application. Case Rep Pediatr. 2012;2012:491692.

  [2]. mepivacaine hydrochloride.

  [3]. Burm, A.G., et al., Pharmacokinetics of the enantiomers of mepivacaine after intravenous administration of the racemate in volunteers. Anesth Analg, 1997. 84(1): p. 85-9.

  [4]. Leffler, A., J. Reckzeh, and C. Nau, Block of sensory neuronal Na+ channels by the secreolytic ambroxol is associated with an interaction with local anesthetic binding sites. Eur J Pharmacol, 2010. 630(1-3): p. 19-28.

MSDS

Material Safety Data Sheet Section1. Identification of the substance Product Name: Mepivacaine Synonyms: Section2. Hazards identification Harmful by inhalation, in contact with skin, and if swallowed. Section3. Composition/information on ingredients. Ingredient name:Mepivacaine CAS number:96-88-8 Section4. First aid measures Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing contaminated clothing and shoes. If irritation persists, seek medical attention. Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical attention. Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention. Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention. Section5. Fire fighting measures In the event of a fire involving this material, alone or in combination with other materials, use dry powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus should be worn. Section6. Accidental release measures Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national standards. Respiratory precaution:Wear approved mask/respirator Hand precaution:Wear suitable gloves/gauntlets Skin protection:Wear suitable protective clothing Eye protection:Wear suitable eye protection Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container for disposal. See section 12. Environmental precautions: Do not allow material to enter drains or water courses. Section7. Handling and storage Handling:This product should be handled only by, or under the close supervision of, those properly qualified in the handling and use of potentially hazardous chemicals, who should take into account the fire, health and chemical hazard data given on this sheet. Store in closed vessels. Storage: Section8. Exposure Controls / Personal protection Engineering Controls: Use only in a chemical fume hood. Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles. General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse. Section9. Physical and chemical properties Appearance:Not specified Boiling point:No data No data Melting point: Flash point:No data Density:No data Molecular formula:C15H22N2O Molecular weight:246.4 Section10. Stability and reactivity Conditions to avoid: Heat, flames and sparks. Materials to avoid: Oxidizing agents. Possible hazardous combustion products: Carbon monoxide, nitrogen oxides. Section11. Toxicological information No data. Section12. Ecological information No data. Section13. Disposal consideration Arrange disposal as special waste, by licensed disposal company, in consultation with local waste disposal authority, in accordance with national and regional regulations. Section14. Transportation information Non-harzardous for air and ground transportation. Section15. Regulatory information No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302, or have known CAS numbers that exceed the threshold reporting levels established by SARA Title III, Section 313. SECTION 16 - ADDITIONAL INFORMATION N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TK6300000 CHEMICAL NAME : 2',6'-Pipecoloxylidide, 1-methyl- CAS REGISTRY NUMBER : 96-88-8 BEILSTEIN REFERENCE NO. : 0211230 LAST UPDATED : 199701 DATA ITEMS CITED : 12 MOLECULAR FORMULA : C15-H22-N2-O MOLECULAR WEIGHT : 246.39 WISWESSER LINE NOTATION : T6NTJ A1 BVMR B1 F1 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 : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,845,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 500 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 31,273,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 30 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARVPAX Annual Review of Pharmacology. (Palo Alto, CA) V.1-15, 1961-75. For publisher information, see ARPTDI. Volume(issue)/page/year: 9,503,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,845,1982 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 135 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - tremor REFERENCE : TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 9,38,1962 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 270 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AANEAB Acta Anaesthesiologica Scandinavica. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.1- 1957- Volume(issue)/page/year: 9,1,1965 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 35 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 31,273,1972 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 53 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 31,273,1972 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 6 mg/kg SEX/DURATION : female 11 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - behavioral REFERENCE : NTOTDY Neurobehavioral Toxicology and Teratology. (Fayetteville, NY) V.3-8, 1981-86. For publisher information, see NETEEC. Volume(issue)/page/year: 8,61,1986 *** REVIEWS *** TOXICOLOGY REVIEW BNYMAM Bulletin of the New York Academy of Medicine. (New York Academy of Medicine, 2 E. 103rd St., New York, NY 10029) Ser 2: V.1- 1925- Volume(issue)/page/year: 52,222,1976 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5788 No. of Facilities: 13 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 545 (estimated) No. of Female Employees: 479 (estimated)

安全

• 危害码 (欧洲): Xi
• 海关编码: 2933399090

合成路线

111562-44-8 ~% 96-88-8

文献：Helvetica Chimica Acta, , vol. 42, p. 1324,1326

98-98-6 ~% 96-88-8

文献：Helvetica Chimica Acta, , vol. 42, p. 1324,1326

39627-98-0 ~% 96-88-8

文献：Helvetica Chimica Acta, , vol. 42, p. 1324,1326

77-78-1 ~% 96-88-8

文献：Acta Chemica Scandinavica (1947-1973), , vol. 11, p. 1183,1184

上下游产品

上游产品  4
111562-44-8 98-98-6 39627-98-0 77-78-1
下游产品  0

海关

海关编码	2933399090
中文概述	2933399090. 其他结构含非稠合吡啶环的化合物. 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	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%