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扑米酮

扑米酮用途

Primidone是GABA受体抑制剂。

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扑米酮名称

[ CAS 号 ]:
125-33-7

[ 中文名 ]:
扑米酮

[ 英文名 ]:
Primidone

[中文别名 ]:

[英文别名 ]:

Prysoline
Primidon
Mysoline
Misodine
MFCD00038662
Sertan
Primidone
EINECS 204-737-0
5-ethyl-5-phenyl-dihydro-pyrimidine-4,6-dione
Mylepsinum

扑米酮生物活性

[ 描述 ]:

Primidone是GABA受体抑制剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

信号通路 >> 神经信号通路 >> GABA受体

研究领域 >> 神经疾病

[参考文献]

[1]. Macdonald, R.L. and K.M. Kelly, Antiepileptic drug mechanisms of action. Epilepsia, 1995. 36 Suppl 2: p. S2-12.

[2]. Calzetti, S., et al., Phenylethylmalonamide in essential tremor. A double-blind controlled study. J Neurol Neurosurg Psychiatry, 1981. 44(10): p. 932-4.

[3]. Perucca, E., et al., A comparative study of the relative enzyme inducing properties of anticonvulsant drugs in epileptic patients. Br J Clin Pharmacol, 1984. 18(3): p. 401-10.

[相关活性小分子]

扑米酮物理化学性质

[ 密度 ]:
1.138g/cm3

[ 沸点 ]:
520.7ºC at 760mmHg

[ 熔点 ]:
281-282°C

[ 分子式 ]:
C₁₂H₁₄N₂O₂

[ 分子量 ]:
218.25200

[ 闪点 ]:
228.2ºC

[ 精确质量 ]:
218.10600

[ PSA ]:
58.20000

[ LogP ]:
1.19550

[ 外观性状 ]:
无气味的白色结晶粉末，略苦味道，无酸性

[ 蒸汽压 ]:
6.08E-11mmHg at 25°C

[ 折射率 ]:
1.528

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
<0.1 g/100 mL at 19 ºC

扑米酮MSDS

扑米酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV9100000

CHEMICAL NAME :: 4,6(1H,5H)-Pyrimidinedione, 5-ethyldihydro-5-phenyl-

CAS REGISTRY NUMBER :: 125-33-7

BEILSTEIN REFERENCE NO. :: 0218034

LAST UPDATED :: 199712

DATA ITEMS CITED :: 33

MOLECULAR FORMULA :: C12-H14-N2-O2

MOLECULAR WEIGHT :: 218.28

WISWESSER LINE NOTATION :: T6MV DVMTJ C2 CR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 38 gm/kg/7Y-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 240 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 - rat

DOSE/DURATION :: >2 gm/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 :: 280 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 332 mg/kg

TOXIC EFFECTS :: Behavioral - anticonvulsant

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 340 mg/kg

TOXIC EFFECTS :: Behavioral - anticonvulsant

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10500 mg/kg/14D-C

TOXIC EFFECTS :: Behavioral - ataxia 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 - rat

DOSE/DURATION :: 17062 mg/kg/13W-C

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 27440 mg/kg/14D-C

TOXIC EFFECTS :: Behavioral - ataxia Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 89 gm/kg/13W-C

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2 gm/kg/4D-I

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10350 mg/kg

SEX/DURATION :: female 1-39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - skin and skin appendages Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10350 mg/kg

SEX/DURATION :: female 1-39 week(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2025 mg/kg

SEX/DURATION :: female 1-39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Effects on Newborn - Apgar score (human only)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 10640 mg/kg

SEX/DURATION :: female 1-38 week(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - drug dependence Reproductive - Effects on Newborn - physical

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 330 mg/kg

SEX/DURATION :: female 6-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 990 mg/kg

SEX/DURATION :: female 6-16 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 875 mg/kg

SEX/DURATION :: male 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 275 mg/kg

SEX/DURATION :: female 6-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

TYPE OF TEST :: Sperm Morphology

MUTATION DATA

TYPE OF TEST :: Micronucleus test

TEST SYSTEM :: Rodent - hamster Embryo

DOSE/DURATION :: 250 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 392,61,1997 *** REVIEWS *** TOXICOLOGY REVIEW DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969- Volume(issue)/page/year: 8,690,1974 TOXICOLOGY REVIEW AUHPAI Australian Journal of Hospital Pharmacy. (B.R. Miller, POB 125, Heidelberg, Vic., Australia) V.1- 1971- Volume(issue)/page/year: 4(1),5,1974 TOXICOLOGY REVIEW DRUGAY Drugs. International Journal of Current Therapeutics and Applied Pharmacology Reviews. (ADIS Press International Inc., Suite B-30, Oxford Ct. Business Center, 582 Middletown Blvd., Langhorne, PA 19047) V.1- 1971- Volume(issue)/page/year: 8,354,1974 TOXICOLOGY REVIEW PRSMA4 Proceedings of the Royal Society of Medicine. (New York, NY) V.1-70, 1907-77. For publisher information, see JRSMD9. Volume(issue)/page/year: 63,48,1970 TOXICOLOGY RIVIEW BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,442,1973 TOXICOLOGY REVIEW AJDCAI American Journal of Diseases of Children. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1-80(3), 1911-50; V.100- 1960- Volume(issue)/page/year: 131,1337,1977 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4105 No. of Facilities: 416 (estimated) No. of Industries: 3 No. of Occupations: 6 No. of Employees: 11085 (estimated) No. of Female Employees: 6869 (estimated)

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扑米酮安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H351

[ 警示性声明 ]:
P280-P301 + P312 + P330

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S22-S36-S45

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ RTECS号 ]:
UV9100000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

扑米酮合成路线

扑米酮上下游产品

扑米酮上游产品

扑米酮下游产品

扑米酮制备

生产方法简述：将乙酸乙酯加入乙醇钠中，回流半小时，冷却至室温，加入乙基苯基丙二酸二乙酯及硫脲，加流9h。冷至0℃，加入乙醇，在0-5℃滴入盐酸至pH=3-3.5。加入锌粉，升温至回流，缓缓补加盐酸，保持的应液有2-3%含酸量，加毕，保温3h。趁热过滤，滤液回收乙醇。冷至20℃，加水，过滤，洗涤滤饼，得成品。

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扑米酮文献

Optimized removal of dissolved organic carbon and trace organic contaminants during combined ozonation and artificial groundwater recharge.

Water Res. 46(18) , 6059-68, (2012)

Pilot scale experiments using an 8 g/h ozonation unit and a 1.4 m(2) slow sand filter have demonstrated that the combination of ozonation and artificial groundwater recharge is suitable for efficient ...

Carrier Mediated Distribution System (CAMDIS): a new approach for the measurement of octanol/water distribution coefficients.

Eur. J. Pharm. Sci. 68 , 68-77, (2015)

Here we present a miniaturized assay, referred to as Carrier-Mediated Distribution System (CAMDIS) for fast and reliable measurement of octanol/water distribution coefficients, log D(oct). By introduc...

How did phenobarbital's chemical structure affect the development of subsequent antiepileptic drugs (AEDs)?

Epilepsia 53 Suppl 8 , 3-11, (2012)

Phenobarbital has been in clinical use as an antiepileptic drug (AED) since 1912. The initial clinical success of phenobarbital and other barbiturates affected the design of subsequent AEDs (e.g., phe...

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扑米酮

扑米酮用途

扑米酮名称

扑米酮生物活性

扑米酮物理化学性质

扑米酮MSDS

详细MSDS(安全技术说明书)

扑米酮毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

扑米酮安全信息

扑米酮合成路线

详细合成路线

扑米酮上下游产品

扑米酮上游产品

扑米酮下游产品

扑米酮制备

扑米酮文献

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