奥沙米特
奥沙米特用途
奥沙米特名称
[ CAS 号 ]:
60607-34-3
[ 中文名 ]:
奥沙米特
[ 英文名 ]:
Oxatomide
[中文别名 ]:
[英文别名 ]:
- Oxatomidum
- MFCD00211147
- KW-4354
- EINECS 262-320-9
- Oxatomida
- Oxatomidum [INN-Latin]
- oxatomide
- Oxetal
- Tinset
- Oxatimide
奥沙米特生物活性
[ 描述 ]:
[ 相关类别 ]:
[ 靶点 ]
H1 Receptor
P2X7
serotonin
[参考文献]
奥沙米特物理化学性质
[ 密度 ]:
1.175 g/cm3
[ 沸点 ]:
621.1ºC at 760 mmHg
[ 熔点 ]:
153.60C
[ 分子式 ]:
C27H30N4O
[ 分子量 ]:
426.55300
[ 闪点 ]:
329.4ºC
[ 精确质量 ]:
426.24200
[ PSA ]:
44.27000
[ LogP ]:
4.00270
[ 外观性状 ]:
白色粉末
[ 折射率 ]:
1.619
[ 储存条件 ]:
Refrigerator
[ 水溶解性 ]:
DMSO: soluble
奥沙米特MSDS
奥沙米特毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- DE2276000
- CHEMICAL NAME :
- 2H-Benzimidazol-2-one, 1,3-dihydro-1-(3-(4-(diphenylmethyl)-1-piperazinyl)pr opyl)-
- CAS REGISTRY NUMBER :
- 60607-34-3
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 19
- MOLECULAR FORMULA :
- C27-H30-N4-O
- MOLECULAR WEIGHT :
- 426.61
- WISWESSER LINE NOTATION :
- T56 BMVNJ D3- AT6N DNTJ DYR&R
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 :
- 1410 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 63 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >4500 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 29 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 9596 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 7926 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >10125 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 25 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 320 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 3,465,1978
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 23 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 3,465,1978 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 4800 mg/kg/30D-I
- TOXIC EFFECTS :
- Liver - changes in liver weight Kidney, Ureter, Bladder - urine volume increased Endocrine - changes in thyroid weight
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 14400 mg/kg/26W-I
- TOXIC EFFECTS :
- Liver - other changes Kidney, Ureter, Bladder - urine volume increased
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2769,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 2400 mg/kg/30D-I
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2805,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 3600 mg/kg/26W-I
- TOXIC EFFECTS :
- Behavioral - tremor Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - nausea or vomiting
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2805,1984 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 110 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2851,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 840 mg/kg
- SEX/DURATION :
- female 14 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2851,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 440 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2851,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 100 mg/kg
- SEX/DURATION :
- female 19-22 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 12,2851,1984
奥沙米特安全信息
[ 符号 ]:
GHS07
[ 信号词 ]:
Warning
[ 危害声明 ]:
H302
[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves
[ 危害码 (欧洲) ]:
Xn: Harmful;
[ 风险声明 (欧洲) ]:
R22
[ 安全声明 (欧洲) ]:
26-36
[ 危险品运输编码 ]:
NONH for all modes of transport
[ WGK德国 ]:
3
[ RTECS号 ]:
DE2276000
[ 海关编码 ]:
2933990090
奥沙米特合成路线
奥沙米特上下游产品
奥沙米特上游产品
奥沙米特下游产品
奥沙米特制备
将5.3份1-(3-氯丙基)-2H-苯并咪唑-2-酮,5份1-(二苯甲基)哌嗪,6.4份碳酸氢钠和200份4-甲基-2-戊酮,一起搅拌回流过夜,反应生成奥沙米特,经分离提纯而得成品。
邻苯二胺、乙酰乙酸乙酯和氢氧化钾醇溶液溶于二甲苯,回流脱水。浓缩,冷至4℃。滤集固体,水洗,干燥,得化合物(I),收率82%。
化合物(I)、1-溴-3-氯丙烷、氢氧化钾和PEG-400溶于甲苯,回流。倾出甲苯溶液,加入10mol/L硫酸,室温水解。加水,再搅拌。滤除沉淀,滤液水洗至中性,干燥。蒸干得化合物(Ⅱ),收率74%。
N-二苯甲基哌嗪、化合物(Ⅱ)、三乙胺和碘化钾溶于甲苯,回流。加入甲苯和水,搅拌。分去水层,甲苯层水洗,干燥,过滤,蒸干。残物用95%乙醇重结晶,得白色固体的奥沙米特,收率51.5%,熔点153℃。
奥沙米特海关
[ 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%
奥沙米特文献
Drugs 69(18) , 2541-76, (2009)
Allergic rhinitis (AR) affects a large percentage of paediatric patients. With the wide array of available agents, it has become a challenge to choose the most appropriate treatment for patients. Seco...
Differential thermodynamic driving force of first- and second-generation antihistamines to determine their binding affinity for human H1 receptors.Biochem. Pharmacol. 91(2) , 231-41, (2014)
Differential binding sites for first- and second-generation antihistamines were indicated on the basis of the crystal structure of human histamine H1 receptors. In this study, we evaluated differences...
Molecular complexes of ketaconazole and oxatomide with p-chloranil: spectroscopic and spectrofluorimetric studies.Spectrochim. Acta. A. Mol. Biomol. Spectrosc. 79(5) , 1137-44, (2011)
The molecular complexes of the donors ketaconazole (KTZ) and oxatomide (OXA) drugs with 2,3,5,6-tetrachloro-1,4-benzoquinone (p-chloranil, p-CHL) have been investigated spectroscopically (UV-vis, FT-I...
推荐生产厂家/供应商:
公司名:上海阿拉丁生化科技股份有限公司
区域:上海市浦东新区
价格:
¥1354.0/10mg
¥需询单/1g
¥需询单/1g
¥需询单/1g
联系人:阿拉丁李高志
产品详情:Oxatomide
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相关化合物
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