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安乃近

安乃近用途

Metamizole sodium 是一种非阿片化合物,具有良好的镇痛、解热的效果。Metamizole sodium 是一种环氧合酶-3 (COX-3) 抑制剂。

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安乃近名称

[ CAS 号 ]:
68-89-3

[ 中文名 ]:
安乃近

[ 英文名 ]:
Metamizole sodium

[中文别名 ]:

[英文别名 ]:

narone
Novil
Magnopyrol
Methamizole Sodium
pyrojec
conmel
Novacid
Sulpin
Unagen
fevonil

安乃近生物活性

[ 描述 ]:

Metamizole sodium 是一种非阿片化合物,具有良好的镇痛、解热的效果。Metamizole sodium 是一种环氧合酶-3 (COX-3) 抑制剂。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

研究领域 >> 神经疾病

[ 靶点 ]

COX-3[2]

[体外研究]

安乃近钠抑制COX-3的IC50值为52μM和COX-1在昆虫细胞中的浓度高出6.6倍[2]。安乃近(1-500)μ米；48小时)显著抑制胰腺癌细胞的细胞增殖[3]。细胞增殖试验[3]细胞系：胰腺癌细胞系PaTu 8988t和Panc-1浓度：1μM、 10个μM、 100个μM、 250个μM、 500个μM孵育时间：48h结果：显著抑制patu8988t细胞增殖；在胰腺癌细胞系Panc-1的1-250处显著抑制细胞增殖μM。

[体内研究]

安乃近钠(500mg/kg；i、 p。；一天两次；7天)减少大鼠神经病理性疼痛症状的发展[4]。动物模型：雄性Wistar大鼠(270-300 g),周围神经病理性疼痛[4]剂量：500 mg/kg给药：腹腔注射,每天2次,连续7天结果：坐骨神经损伤后7天,DRG内促痛性白细胞介素(IL-1β,IL-6,IL-18)和趋化因子(CCL2,CCL4,CCL7)的表达降低。

[参考文献]

[1]. A Jasiecka, et al. Pharmacological characteristics of metamizole. Pol J Vet Sci. 2014;17(1):207-14.

[2]. N V Chandrasekharan, et al. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: cloning, structure, and expression. Proc Natl Acad Sci U S A. 2002 Oct 15; 99(21): 13926–13931.

[3]. Manuela Malsy, et al. Effects of metamizole, MAA, and paracetamol on proliferation, apoptosis, and necrosis in the pancreatic cancer cell lines PaTu 8988 t and Panc-1. BMC Pharmacol Toxicol. 2017 Dec 6;18(1):77.

[4]. Renata Zajaczkowska, et al. Metamizole relieves pain by influencing cytokine levels in dorsal root ganglia in a rat model of neuropathic pain. Pharmacol Rep. 2020 Oct;72(5):1310-1322.

安乃近物理化学性质

[ 熔点 ]:
187ºC

[ 分子式 ]:
C₁₃H₁₆N₃NaO₄S

[ 分子量 ]:
333.339

[ 精确质量 ]:
333.075928

[ PSA ]:
95.75000

[ LogP ]:
1.50410

[ 外观性状 ]:
白色或淡黄色结晶粉末

[ 储存条件 ]:
库房通风低温干燥

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
水溶性：可溶

安乃近MSDS

详细MSDS(安全技术说明书)

安乃近毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: PB1300000

CHEMICAL NAME :: Methanesulfonic acid, (antipyrinylmethylamino)-, monosodium salt

CAS REGISTRY NUMBER :: 68-89-3

LAST UPDATED :: 199607

DATA ITEMS CITED :: 37

MOLECULAR FORMULA :: C13-H17-N3-O4-S.Na

MOLECULAR WEIGHT :: 334.38

WISWESSER LINE NOTATION :: T5NNVJ A1 BR& D1M1SWQ E1

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 :: 3 gm/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LC - Lethal concentration

ROUTE OF EXPOSURE :: Inhalation

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >900 mg/m3

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2470 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2117 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2182 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1625 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2891 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LC50 - Lethal concentration, 50 percent kill

ROUTE OF EXPOSURE :: Inhalation

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 37200 mg/m3

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 250 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 69 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2197 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2750 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2150 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 61800 mg/kg/30D-I

TOXIC EFFECTS :: Endocrine - changes in spleen weight Blood - pigmented or nucleated red blood cells Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: TCLo - Lowest published toxic concentration

ROUTE OF EXPOSURE :: Inhalation

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 192 mg/m3/4H/30D-I

TOXIC EFFECTS :: Behavioral - alteration of classical conditioning Liver - liver function tests impaired

TYPE OF TEST :: TCLo - Lowest published toxic concentration

ROUTE OF EXPOSURE :: Inhalation

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 20 mg/m3/4H/17W-I

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS Blood - change in clotting factors Nutritional and Gross Metabolic - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 45500 mg/kg/13W-C

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 gm/kg/30D-C

TOXIC EFFECTS :: Blood - changes in erythrocyte (RBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 gm/kg/30D-C

TOXIC EFFECTS :: Blood - normocytic anemia Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 6300 mg/kg/30D-I

TOXIC EFFECTS :: Endocrine - other changes Blood - changes in other cell count (unspecified)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 536 mg/kg/78W-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Liver - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 792 mg/kg/78W-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30 mg/kg

SEX/DURATION :: lactating female 41 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - other neonatal measures or effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 750 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1 gm/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Fibroblast

DOSE/DURATION :: 750 mg/L

REFERENCE :: ESKHA5 Eisei Shikenjo Hokoku. Bulletin of the Institute of Hygienic Sciences. (Kokuritsu Eisei Shikenjo Kagaku, 18-1 Bushitsu Johobu, Setagaya-ku, Tokyo 158, Japan) V.1- 1886- Volume(issue)/page/year: (96),55,1978 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-RUSSIA:STEL 0.5 mg/m3 JAN 1993

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安乃近安全信息

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R42/43

[ 安全声明 (欧洲) ]:
S36

[ WGK德国 ]:
2

[ RTECS号 ]:
PB1300000

[ 海关编码 ]:
2933192000

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安乃近海关

[ 海关编码 ]: 2933192000

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安乃近