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瑞吡司特

瑞吡司特用途

雷普利司(MY-5116)是一种口服活性抗过敏药物。雷普利司特抑制组胺释放。雷普利司特可用于支气管哮喘的研究[1][2][3]。
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瑞吡司特名称

[ CAS 号 ]:
73080-51-0

[ 中文名 ]:
瑞吡司特

[ 英文名 ]:
Repirinast

[中文别名 ]:

[英文别名 ]:

瑞吡司特生物活性

[ 描述 ]:

雷普利司(MY-5116)是一种口服活性抗过敏药物。雷普利司特抑制组胺释放。雷普利司特可用于支气管哮喘的研究[1][2][3]。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他
研究领域 >> 炎症/免疫

[体外研究]

雷普利司特抑制抗原(IC50:0.3μM)诱导的大鼠腹膜肥大细胞释放组胺[3]。

[体内研究]

雷普利司特(30 mg/kg,i.p.)抑制豚鼠抗原诱导的早期和晚期肺反应[1]。雷普利司特(30 mg/kg,p.o.)抑制大鼠抗原诱导的即刻支气管收缩[2]。动物模型：豚鼠[1]剂量：30 mg/kg给药：腹腔注射(i.p.)结果：抑制白细胞(主要是嗜酸性粒细胞)渗入支气管组织。阻断抗原诱导气道对吸入乙酰胆碱的高反应性。动物模型：哮喘大鼠(10 mg/kg抗原OVA激发)[1]剂量：30 mg/kg给药：口服(p.o.)结果：抑制激发后30秒和1分钟的呼吸次数减少。

[参考文献]

[1]. N Yamada, et al. Repirinast inhibits antigen-induced early and late pulmonary responses and airway hyperresponsiveness in guinea pigs. Int Arch Allergy Immunol. 1993;100(4):367-72.

[2]. Takahashi K. Effects of MY-5116 on experimental asthma in rats and guinea pigs. Arerugi. 1986 Oct; 35(10): 1037-46.

[3]. M Takei, et al. Inhibition of histamine release from rat peritoneal mast cells by MY-1250, an active metabolite of Repirinast (MY-5116). Int Arch Allergy Appl Immunol. 1990;93(2-3):237-41.

瑞吡司特物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
461.1±55.0 °C at 760 mmHg

[ 熔点 ]:
236-241°

[ 分子式 ]:
C8H11N7O

[ 分子量 ]:
221.219

[ 闪点 ]:
232.6±31.5 °C

[ 精确质量 ]:
221.102509

[ PSA ]:
89.37000

[ LogP ]:
0.46

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.731

瑞吡司特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UQ1377000
CHEMICAL NAME :
4H-Pyrano(3,2-c)quinoline-2-carboxylic acid, 5,6-dihydro-7,8-dimethyl-4,5-dioxo-, isopentyl ester
CAS REGISTRY NUMBER :
73080-51-0
LAST UPDATED :
199612
DATA ITEMS CITED :
9
MOLECULAR FORMULA :
C20-H21-N-O5
MOLECULAR WEIGHT :
355.42

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 :
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: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2783 mg/kg
TOXIC EFFECTS :
Gastrointestinal - peritonitis 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: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Skin and Appendages - dermatitis, other (after systemic exposure) 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: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
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: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1435 mg/kg
TOXIC EFFECTS :
Gastrointestinal - peritonitis 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: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Skin and Appendages - dermatitis, other (after systemic exposure) 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: 17,545,1986
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>5 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: 17,577,1986
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Liver - other changes Kidney, Ureter, Bladder - changes primarily in glomeruli 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: 17,545,1986 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
5200 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Fertility - abortion Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
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: 17,51,1986
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瑞吡司特安全信息

[ 海关编码 ]:
2934999090

瑞吡司特合成路线

详细合成路线

瑞吡司特上下游产品

瑞吡司特上游产品

瑞吡司特下游产品

瑞吡司特制备

下列酸化合物转化为酰氯后，再和3-甲基正丁醇在90-100℃下搅拌，得到瑞吡司特。

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瑞吡司特海关

[ 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%

相关化工产品/化学物质：

相关药品：

推荐生产厂家/供应商：

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Repirinast

公司名：武汉壹加壹生物科技有限公司

区域：武汉市江夏区

价格：
￥需询单/1mg

联系人：刘经理

产品详情：瑞吡司特

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