27060-91-9

• 常用中文名：氟恶唑兰
• 常用英文名：Flutazolam
• CAS号：27060-91-9
• 分子式：C₁₉H₁₈ClFN₂O₃
• 分子量：376.80900
• 相关类别： 研究领域 神经疾病
• 发布时间：2018-09-06 12:07:21
• 更新时间：2024-01-05 07:40:14
• Flutazolam (MS 4101; Ro 7-6102) 是一种药物,作用于大脑的苯二氮卓类受体,可缓解焦虑或紧张。

名称

• 中文名: 氟恶唑兰
• 英文名: 10-chloro-11b-(2-fluorophenyl)-7-(2-hydroxyethyl)-3,5-dihydro-2H-[1,3]oxazolo[3,2-d][1,4]benzodiazepin-6-one
• 英文别名: 10-Chloro-11b-(o-fluorophenyl)-2,3,7,11b-tetrahydro-7-(2-hydroxyethyl)oxazolo(3,2-d)(1,4)benzodiazepin-6(5H)-one; Oxazolo(3,2-d)(1,4)benzodiazepin-6(5H)-one,10-chloro-11b-(o-fluorophenyl)-2,3,7,11b-tetrahydro-7-(2-hydroxyethyl); 10-Chloro-11b-(2-fluorophenyl)-7-(2-hydroxyethyl)-2,3,5,11b-tetrahydrooxazolo[3,2-d][1,4]benzodiazepin-6(7H)-one; MS-4101; flutazolam; Flutazolam [INN:JAN]; Flutazolamum [INN-Latin]; 10-Chloro-11b-(2-fluorophenyl)-2,3,7,11b-tetrahydro-7-(2-hydroxyethyl)oxazolo(3,2-d)(1,4)benzodiazepin-6(5H)-one; Flutazolamum

物化性质

• 密度: 1.47g/cm3
• 沸点: 601.9ºC at 760mmHg
• 分子式: C₁₉H₁₈ClFN₂O₃
• 分子量: 376.80900
• 闪点: 317.8ºC
• 精确质量: 376.09900
• PSA: 53.01000
• LogP: 2.35420
• 蒸汽压: 2.44E-15mmHg at 25°C
• 折射率: 1.672

生物活性

• 描述: Flutazolam (MS 4101; Ro 7-6102) 是一种药物,作用于大脑的苯二氮卓类受体,可缓解焦虑或紧张。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 靶点:

  Benzodiazepine receptor[1]

• 体外研究: MS-4101抑制隔膜大鼠的高度运动,长期离体小鼠的抗击行为和戊四唑惊厥,加强硫喷妥钠睡眠。 MS-4101的这些效果与地西泮的效力相同。 MS-4101显着抑制小鼠中由mescaline引起的刮擦和头部抽搐[1]。
• 参考文献:

  [1]. Mitsushima T, et al. Psychopharmacological effects of flutazolam (MS-4101). Nihon Yakurigaku Zasshi. 1978 Nov;74(8):959-79.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RQ5831400 CHEMICAL NAME : Oxazolo(3,2-d)(1,4)benzodiazepin-6(5H)-one, 10-chloro-11b-(o-fluorophenyl)- 2,3,7,11b-tetrahydro-7-(2-hydroxyethyl)- CAS REGISTRY NUMBER : 27060-91-9 LAST UPDATED : 199612 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C19-H18-Cl-F-N2-O3 MOLECULAR WEIGHT : 376.84 WISWESSER LINE NOTATION : T B576 CO FN HVNTT&J BR BF& I2Q MG 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 : >6 gm/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - body temperature decrease 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: 6,1997,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 4050 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression 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: 6,1997,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >6 gm/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: 6,1997,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1910 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: 6,2335,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1680 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) 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: 6,1997,1978 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - ataxia 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: 6,1997,1978 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 14 gm/kg/5W-C TOXIC EFFECTS : Liver - changes in liver weight Blood - pigmented or nucleated red blood cells Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,693,1978 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1050 mg/kg SEX/DURATION : female 14 day(s) pre-mating female 1-7 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,395,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 80 mg/kg SEX/DURATION : female 8-15 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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: 6,1692,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1500 mg/kg SEX/DURATION : female 17-22 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,395,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 270 mg/kg SEX/DURATION : female 17-22 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - behavioral REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,395,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 13 gm/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,709,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 3250 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,709,1978

合成路线

24143-22-4 540-51-2 ~% 27060-91-9

文献：Hoffmann-La Roche Inc. Patent: US3965151 A1, 1976 ;

105-36-2 24143-22-4 ~% 27060-91-9

文献：Hoffmann-La Roche Inc. Patent: US3965151 A1, 1976 ;

102408-32-2 ~% 27060-91-9

文献：Kuruno; Kamiya; Kuwayama; Jinno; Yashiro; Ikeda Chemical and Pharmaceutical Bulletin, 1987 , vol. 35, # 9 p. 3831 - 3837

101489-22-9 ~% 27060-91-9

文献：Kuwayama; Kurono; Muramatsu; Yashiro; Ikeda Chemical and Pharmaceutical Bulletin, 1986 , vol. 34, # 1 p. 320 - 326

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