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拉呋替丁

拉呋替丁用途

消化系统用药物

拉呋替丁名称

[ CAS 号 ]:
118288-08-7

[ 中文名 ]:
拉呋替丁

[ 英文名 ]:
Lafutidine

[中文别名 ]:

拉夫替丁

[英文别名 ]:

(z)-inyl)oxy)-2-butenyl)
LAFUTIDINE(SUBJECTTOPATENTFREE)
Protecadin
Stogar
Laflutidine
lafutidine
enyl)acetamide
MFCD00867520

拉呋替丁生物活性

[ 描述 ]:

Lafutidine是新型的H2受体拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 代谢疾病

[参考文献]

[1]. Tanaka M, et al. Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86.

[相关活性小分子]

拉呋替丁物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
704.2±60.0 °C at 760 mmHg

[ 熔点 ]:
99 °C

[ 分子式 ]:
C₂₂H₂₉N₃O₄S

[ 分子量 ]:
431.548

[ 闪点 ]:
379.7±32.9 °C

[ 精确质量 ]:
431.187866

[ PSA ]:
103.88000

[ LogP ]:
1.10

[ 外观性状 ]:
固体;White to Orange to Green powder to crystal

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.599

[ 储存条件 ]:
室温，干燥，密封

[ 水溶解性 ]:
水溶性：不溶；易溶于：二甲基甲酰胺；可溶于：甲醇；极微溶：乙醚,甲醇

拉呋替丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AC2957000

CHEMICAL NAME :: Acetamide, 2-((2-furanylmethyl)sulfinyl)-N-(4-((4-(1-piperidinyl methyl)-2-pyridinyl)o xy)- 2-butenyl)-, (Z)-

CAS REGISTRY NUMBER :: 118288-08-7

LAST UPDATED :: 199607

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C22-H29-N3-O4-S

MOLECULAR WEIGHT :: 431.60

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 :: 1248 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,143,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 84 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,143,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1034 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,143,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 47900 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,143,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >400 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,417,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 36400 mg/kg/52W-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,167,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9100 mg/kg/13W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,149,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 gm/kg/2W-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,149,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 9100 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Blood - other changes Related to Chronic Data - death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,421,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 10920 mg/kg/52W-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 50,439,1995

拉呋替丁安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36/37/39

[ 海关编码 ]:
2929909090

拉呋替丁合成路线

详细合成路线

拉呋替丁上下游产品

拉呋替丁上游产品

拉呋替丁下游产品

拉呋替丁制备

将氢化钠悬浮于四氢呋喃中，在室温滴加(Z)-4-四氢吡喃氧基-2-丁烯醇的四氢呋喃溶液，搅拌，依次加入2-氯-4-哌啶基甲基吡啶和二甲基甲酰胺，反应完毕，经处理得到(Z)-4-哌啶基甲基-2-(4-四氢吡啶氧基-2-丁烯-氧基)吡啶。该化合物溶于甲醇，在冰浴冷却下，加入对甲苯磺酸单水合物，搅拌反应，经处理得到(Z)-4-[4-(哌啶基甲基)吡啶-2-氧基]-2-丁烯醇。该化合物和三乙胺溶于甲苯，在冰浴冷却下滴加甲磺酰氯的甲苯溶
液，搅拌，经处理得到溶液。在2-呋喃甲基亚磺酰基乙酰胺的甲苯溶液中加入叔丁氧钾，滴加上面得到的溶液反应，经处理得到拉呋替丁。

拉呋替丁海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%