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瑞巴派特

瑞巴派特用途

Rebamipide是内源性前列腺素诱导剂,同时是自由基清除剂。

瑞巴派特名称

[ CAS 号 ]:
90098-04-7

[ 中文名 ]:
瑞巴匹特

[ 英文名 ]:
Rebamipide

[中文别名 ]:

瑞巴派特

[英文别名 ]:

1H-benzimidazol-2-yl(4-chlorophenyl)methanone
Mucosta
Proamipide
REBAMIPIDEREBAMIPIDE
REACTIVE ORANGE 122,CINO.ORANGE 122
MFCD00866895
2-(4-chlorobenzoyl)benzimidazole
Rebamipide

瑞巴派特生物活性

[ 描述 ]:

Rebamipide是内源性前列腺素诱导剂,同时是自由基清除剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

研究领域 >> 代谢疾病

[参考文献]

[1]. Iinuma, S., et al., In vitro studies indicating antioxidative properties of rebamipide. Dig Dis Sci, 1998. 43(9 Suppl): p. 35S-39S.

[2]. Arakawa, T., et al., Rebamipide: overview of its mechanisms of action and efficacy in mucosal protection and ulcer healing. Dig Dis Sci, 1998. 43(9 Suppl): p. 5S-13S.

[3]. Arakawa, T., et al., Rebamipide, novel prostaglandin-inducer accelerates healing and reduces relapse of acetic acid-induced rat gastric ulcer. Comparison with cimetidine. Dig Dis Sci, 1995. 40(11): p. 2469-72.

[相关活性小分子]

瑞巴派特物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
695.0±55.0 °C at 760 mmHg

[ 熔点 ]:
288-290ºC dec.

[ 分子式 ]:
C₁₉H₁₅ClN₂O₄

[ 分子量 ]:
370.786

[ 闪点 ]:
374.1±31.5 °C

[ 精确质量 ]:
370.072021

[ PSA ]:
99.26000

[ LogP ]:
2.90

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±2.3 mmHg at 25°C

[ 折射率 ]:
1.634

[ 储存条件 ]:
-20°C Freezer

瑞巴派特MSDS

详细MSDS(安全技术说明书)

瑞巴派特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VC2518500

CHEMICAL NAME :: 4-Quinolinepropanoic acid, 1,2-dihydro-alpha-((4-chlorobenzoyl)amino)-2-oxo-, (+-)-

CAS REGISTRY NUMBER :: 90098-04-7

LAST UPDATED :: 199112

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C19-H15-Cl-N2-O4

MOLECULAR WEIGHT :: 370.81

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5 gm/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 700 mg/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Kidney, Ureter, Bladder - other changes

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2637 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - other changes Skin and Appendages - hair

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 572 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Kidney, Ureter, Bladder - other changes

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1353 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - respiratory depression Blood - changes in spleen

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >3 gm/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,362,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 26 gm/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,478,1989

瑞巴派特安全信息

[ 海关编码 ]:
2933790090

瑞巴派特合成路线

详细合成路线

瑞巴派特上下游产品

瑞巴派特上游产品

瑞巴派特下游产品

瑞巴派特制备

1．消旋瑞巴派特的制备。以2(1H)-喹啉酮-4-羧酸甲酯(I)为原料，经氢硼化锂还原为2(1H)-喹啉-4-基甲醇(II)，再和氢溴酸作用溴化为4-溴甲基-2(1H)-喹啉酮(Ⅲ)。
乙酰氨基丙二酸二乙酯(12.0g，55mmo1)和金属钠(1.5g，65mmo1)溶于150ml无水乙醇，加热至沸，在搅拌下加入(Ⅲ)(12.0g，50mmo1)，再回流2h。减压浓缩，剩余物倾入水。过滤收集析出的沉淀，用乙醇重结晶，得13.0g无色棱状结晶的化合物(Ⅳ)，收率69%，熔点224～226℃(分解)。
化合物(Ⅳ)(5.0g，13mmo1)悬浮于150ml 20%盐酸，回流9h。减压浓缩至干，剩余物用乙醇-水重结晶，得3.2g无色棱状结晶的化合物(V)，收率89%，熔点220～225℃(分解)。
化合物(V)(2.7g，10mmo1)和碳酸钾(4.2g，30mmo1)溶于100rnl丙酮和20ml水的混合溶液，在冰浴冷却和搅拌下，滴入对氯苯甲酰氯(2.1g，12mmo1)，再搅拌2h。减压蒸去丙酮，剩余液用稀盐酸酸化。过滤收集析出的沉淀，用甲醇-水重结晶，得1.8g白色粉末状的瑞巴派特，收率49%，熔点288～290℃(分解)。
2．(-)-构型的制备。从消旋体拆分而得。21.6g消旋瑞巴派特悬浮于1100ml甲醇，加入23g(-)-二甲马钱子碱(brucine)，形成的澄清溶液在室温下搅拌4h，再冷却过夜。过滤收集析出的沉淀，用冷甲醇洗。再重结晶4次得7.6g纯的盐，[α]_D²⁰+60.4°(C=1.0，氯仿)。将10%盐酸加到该盐的甲醇悬浮液中，过滤析出的沉淀，用水洗。然后用二甲基甲酰胺-水重结晶3次，得1.6g无色针状结晶的(-)-构型的瑞巴派特，收率14.8%，熔点305～306℃，[α]_D²⁰-116.7°(C=1.0，二甲基甲酰胺)。
3．(+)-构型的制备。将从上述(-)-构型的制备中第1次母液中得到的固体溶于甲醇，加入10%盐酸。过滤析出的沉淀，水洗后，悬浮于甲醇，再加入(-)-二甲马钱子碱，在室温搅拌1h。过滤除去不溶物，往滤液中加入浓盐酸。过滤收集析出的沉淀，水洗。用二甲基甲酰胺-水重结晶4次，得3g无色针状结晶的(+)一构型的瑞巴派特，收率27.8%，熔点305～306℃(分解)，[α]_D²⁰+116.9°(C=1.0，二甲基甲酰胺)。

瑞巴派特海关

[ 海关编码 ]: 2933499090

[ 中文概述 ]:
2933499090. 其他含喹琳或异喹啉环系的化合物〔但未进一步稠合的〕. 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 ]:
2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%