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别嘌醇

别嘌醇用途

Allopurinol (Zyloprim)是黄嘌呤氧化酶(XO)抑制剂,IC50为7.82±0.12 μM。

别嘌醇名称

[ CAS 号 ]:
315-30-0

[ 中文名 ]:
别嘌醇

[ 英文名 ]:
Allopurinol

[中文别名 ]:

[英文别名 ]:

Urosin
Urbol
7H-Pyrazolo[3,4-d]pyrimidin-4-ol
Apurol
Pural
1,5-Dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
Anoprolin
HPP
Sigapurol
allopurinal

别嘌醇生物活性

[ 描述 ]:

Allopurinol (Zyloprim)是黄嘌呤氧化酶(XO)抑制剂,IC50为7.82±0.12 μM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 黄嘌呤氧化酶

研究领域 >> 代谢疾病

[参考文献]

[1]. Pacher P, et al. Therapeutic effects of xanthine oxidase inhibitors: renaissance half a century after the discovery of allopurinol. Pharmacol Rev. 2006 Mar;58(1):87-114.

[2]. Reiter S, et al. Demonstration of a combined deficiency of xanthine oxidase and aldehyde oxidase in xanthinuric patients not forming oxipurinol. Clin Chim Acta. 1990 Mar 15;187(3):221-34.

[相关活性小分子]

别嘌醇物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
290.8ºC at 760 mmHg

[ 熔点 ]:
350 ºC

[ 分子式 ]:
C₅H₄N₄O

[ 分子量 ]:
136.111

[ 闪点 ]:
129.7ºC

[ 精确质量 ]:
136.038513

[ PSA ]:
74.43000

[ LogP ]:
-1.46

[ 外观性状 ]:
白色至灰白色固体

[ 折射率 ]:
1.816

[ 储存条件 ]:
库房低温,通风,干燥,与食品原料分开存放

[ 水溶解性 ]:
0.35 g/L (25 ºC)

别嘌醇MSDS

别嘌醇毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UR0785000

CHEMICAL NAME :: H-Pyrazolo(3,4-d)pyrimidin-4-ol

CAS REGISTRY NUMBER :: 315-30-0

LAST UPDATED :: 199803

DATA ITEMS CITED :: 19

MOLECULAR FORMULA :: C5-H4-N4-O

MOLECULAR WEIGHT :: 136.13

WISWESSER LINE NOTATION :: T56 BMN GN INJ FQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 42 mg/kg/7D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 76,47,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 120 mg/kg/4W-I

TOXIC EFFECTS :: Blood - other changes Skin and Appendages - dermatitis, allergic (after systemic exposure) Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: CEDEDE Clinical and Experimental Dermatology. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1976- Volume(issue)/page/year: 19,243,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 88 mg/kg/22D-I

TOXIC EFFECTS :: Blood - leukopenia

REFERENCE :: ARDIAO Annals of the Rheumatic Diseases. (British Medical Journal, Box 560B, Kennebunkport, ME 04041) V.1- 1939- Volume(issue)/page/year: 40,245,1981

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 21429 ug/kg/5D-I

TOXIC EFFECTS :: Behavioral - muscle weakness Liver - jaundice, other or unclassified Blood - thrombocytopenia

REFERENCE :: ARDIAO Annals of the Rheumatic Diseases. (British Medical Journal, Box 560B, Kennebunkport, ME 04041) V.1- 1939- Volume(issue)/page/year: 40,245,1981

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >500 mg/kg

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

REFERENCE :: PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 7,735,1973

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 900 mg/kg

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

REFERENCE :: ADTEAS Advances in Teratology. (New York, NY) V.1-5, 1966-72. Discontinued. Volume(issue)/page/year: 3,181,1968

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 78 mg/kg

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

REFERENCE :: PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 7,735,1973

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 214 mg/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Behavioral - fluid intake Behavioral - ataxia

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 64,108,1968

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 298 mg/kg

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

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 23,715,1981

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >100 mg/kg

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

REFERENCE :: PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 7,735,1973 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 300 mg/kg/3D-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 9,343,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1 gm/kg/10D-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 - transaminases

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 9,343,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 300 mg/kg/3D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Metabolism (Intermediary) - xanthine, purine or nucleotides including urate

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 45,271,1987 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 50 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,201,1972

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 100 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,201,1972 *** REVIEWS *** TOXICOLOGY REVIEW INTEAG Internist. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1960- Volume(issue)/page/year: 15,7,1974 TOXICOLOGY REVIEW ARVPAX Annual Review of Pharmacology. (Palo Alto, CA) V.1-15, 1961-75. For publisher information, see ARPTDI. Volume(issue)/page/year: 5,447,1965 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4802 No. of Facilities: 94 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1456 (estimated) No. of Female Employees: 840 (estimated)

别嘌醇安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H317

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P280

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R25;R36/37/38;R43

[ 安全声明 (欧洲) ]:
S28-S36/37-S45-S36/37/39-S26-S24

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
2

[ RTECS号 ]:
UR0785000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2933990090

别嘌醇合成路线

别嘌醇上下游产品

别嘌醇上游产品

别嘌醇下游产品

别嘌醇制备

1.将氰乙酸乙酯、原甲酸三乙酯、乙酐放在反应罐中回流反应4h，缩合得到α-乙氧次甲基氰乙酸乙酯：再将其溶解在乙醇中，加入水合肼，加热回流反应6h，得3-氨基-4-乙氧羰基吡唑；最后与甲酰胺一起加热回流反应8h，环合得到别嘌醇。用蒸馏水溶解，活性炭脱色，得精制的别嘌醇。对氰乙酸乙酯计，总收率41.8%

别嘌醇海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

别嘌醇文献

The efficacy of short and repeated high-pressure processing treatments on the reduction of non-O157:H7 Shiga-toxin producing Escherichia coli in ground beef patties.

Meat Science 102 , 22-6, (2015)

High pressure processing (HPP) has previously been shown to be effective at reducing Escherichia coli O157:H7 in meat products. However, few studies have determined whether HPP may be effective at red...

In vitro Xanthine Oxidase Inhibitory Studies of Lippia nodiflora and Isolated Flavonoids and Phenylethanoid Glycosides as Potential Uric Acid-lowering Agents.

Nat. Prod. Commun. 10 , 945-8, (2015)

Lippia nodiflora has been traditionally used for treatment of knee joint pain. Hitherto, no studies have been reported on the effective use of L. nodiflora against hyperuricemia, gout or other metabol...

Pterostilbene and allopurinol reduce fructose-induced podocyte oxidative stress and inflammation via microRNA-377.

Free Radic. Biol. Med. 83 , 214-26, (2015)

High dietary fructose is an important causative factor in the development of metabolic syndrome-associated glomerular podocyte oxidative stress and injury. Here, we identified microRNA-377 (miR-377) a...

更多文献

别嘌醇相关知识

别嘌醇片-说明书-副作用

2018-12-19 20:38:52

导读：别嘌呤醇（英语：Allopurinol，又名别嘌醇、异嘌呤醇）是主治高尿酸血症（血浆中的尿酸浓度过高）及其并发症痛风病等的药物。别嘌呤醇是一种嘌呤类似物；它是次黄嘌呤（体内一种常见的嘌呤）的异构体且是黄嘌呤氧化酶的酶抑制剂。黄嘌呤氧化酶负责将次黄嘌呤和黄嘌呤的连续氧化，最终产生的产物是尿酸，...

别嘌醇