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27060-91-9

27060-91-9 structure
27060-91-9 structure
  • Name: Flutazolam
  • Chemical Name: 10-chloro-11b-(2-fluorophenyl)-7-(2-hydroxyethyl)-3,5-dihydro-2H-[1,3]oxazolo[3,2-d][1,4]benzodiazepin-6-one
  • CAS Number: 27060-91-9
  • Molecular Formula: C19H18ClFN2O3
  • Molecular Weight: 376.80900
  • Catalog: Research Areas Neurological Disease
  • Create Date: 2018-09-06 12:07:21
  • Modify Date: 2025-08-21 23:12:21
  • Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension.
Name 10-chloro-11b-(2-fluorophenyl)-7-(2-hydroxyethyl)-3,5-dihydro-2H-[1,3]oxazolo[3,2-d][1,4]benzodiazepin-6-one
Synonyms 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
Description Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension.
Related Catalog
Target

Benzodiazepine receptor[1]

In Vitro MS-4101 suppresses hyperemotionality in septal rats, fighting behavior in long-term isolated mice and pentylenetetrazol convulsion and potentiated thiopental sleep. These effects of MS-4101 are the same in potency as those of diazepam. MS-4101 inhibits considerably both scratching and head-twitch induced by mescaline in mice[1].
References

[1]. Mitsushima T, et al. Psychopharmacological effects of flutazolam (MS-4101). Nihon Yakurigaku Zasshi. 1978 Nov;74(8):959-79.
Density 1.47g/cm3
Boiling Point 601.9ºC at 760mmHg
Molecular Formula C19H18ClFN2O3
Molecular Weight 376.80900
Flash Point 317.8ºC
Exact Mass 376.09900
PSA 53.01000
LogP 2.35420
Vapour Pressure 2.44E-15mmHg at 25°C
Index of Refraction 1.672

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
24143-22-4 structure

24143-22-4

540-51-2 structure

540-51-2

~%

27060-91-9 structure

27060-91-9

Literature: Hoffmann-La Roche Inc. Patent: US3965151 A1, 1976 ;
105-36-2 structure

105-36-2

24143-22-4 structure

24143-22-4

~%

27060-91-9 structure

27060-91-9

Literature: Hoffmann-La Roche Inc. Patent: US3965151 A1, 1976 ;
102408-32-2 structure

102408-32-2

~%

27060-91-9 structure

27060-91-9

Literature: Kuruno; Kamiya; Kuwayama; Jinno; Yashiro; Ikeda Chemical and Pharmaceutical Bulletin, 1987 , vol. 35, # 9 p. 3831 - 3837
101489-22-9 structure

101489-22-9

~%

27060-91-9 structure

27060-91-9

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