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甲哌卡因

甲哌卡因用途

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。

甲哌卡因名称

[ CAS 号 ]:
96-88-8

[ 中文名 ]:
2-甲基-2,6-壬二烯-1-胺

[ 英文名 ]:
Mepivacaine

[中文别名 ]:

[英文别名 ]:

甲哌卡因生物活性

[ 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.

甲哌卡因物理化学性质

[ 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

甲哌卡因MSDS

详细MSDS(安全技术说明书)

甲哌卡因毒性和生态

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)

甲哌卡因安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2933399090

甲哌卡因合成路线

详细合成路线

甲哌卡因上下游产品

甲哌卡因上游产品

甲哌卡因下游产品

甲哌卡因海关

[ 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%