flosequinan

Modify Date: 2024-01-09 18:02:18

flosequinan Structure
flosequinan structure
Common Name flosequinan
CAS Number 76568-02-0 Molecular Weight 239.27
Density 1.44g/cm3 Boiling Point 423.1ºC at 760 mmHg
Molecular Formula C11H10FNO2S Melting Point 226-228°
MSDS N/A Flash Point 209.7ºC

 Use of flosequinan


Flosequinan is a balanced vasodilator. Flosequinan not only significantly reduces systemic vascular resistance, but also significantly reduces the beating component of left ventricular afterload, characteristic impedance and arterial wave reflection, which can be used in the research of acute heart failure[1].

 Names

Name 7-fluoro-1-methyl-3-methylsulfinylquinolin-4-one
Synonym More Synonyms

 flosequinan Biological Activity

Description Flosequinan is a balanced vasodilator. Flosequinan not only significantly reduces systemic vascular resistance, but also significantly reduces the beating component of left ventricular afterload, characteristic impedance and arterial wave reflection, which can be used in the research of acute heart failure[1].
Related Catalog
References

[1]. Yano M, et al. Effects of balanced vasodilator, flosequinan, on aortic impedance in failing heart. J Cardiovasc Pharmacol. 1998 Sep;32(3):466-70.  

 Chemical & Physical Properties

Density 1.44g/cm3
Boiling Point 423.1ºC at 760 mmHg
Melting Point 226-228°
Molecular Formula C11H10FNO2S
Molecular Weight 239.27
Flash Point 209.7ºC
Exact Mass 239.04200
PSA 58.28000
LogP 2.28070
Index of Refraction 1.654

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VC8292500
CHEMICAL NAME :
4(1H)-Quinolinone, 7-fluoro-1-methyl-3-(methylsulfinyl)-, (+-)-
CAS REGISTRY NUMBER :
76568-02-0
LAST UPDATED :
199612
DATA ITEMS CITED :
14
MOLECULAR FORMULA :
C11-H10-F-N-O2-S
MOLECULAR WEIGHT :
239.28

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Skin and Appendages - hair
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
120 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
400 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>250 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>1200 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1260 mg/kg/4W-I
TOXIC EFFECTS :
Liver - changes in liver weight Kidney, Ureter, Bladder - urine volume increased Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4095 mg/kg/26W-I
TOXIC EFFECTS :
Liver - fatty liver degeneration Nutritional and Gross Metabolic - changes in sodium Related to Chronic Data - changes in testicular weight
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
18200 mg/kg/52W-I
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands Blood - normocytic anemia Biochemical - Metabolism (Intermediary) - other proteins
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
2800 mg/kg/4W-I
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in adrenal weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
18200 mg/kg/26W-I
TOXIC EFFECTS :
Liver - fatty liver degeneration Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
8190 mg/kg/52W-I
TOXIC EFFECTS :
Cardiac - EKG changes not diagnostic of specified effects Liver - fatty liver degeneration Biochemical - Metabolism (Intermediary) - other proteins
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1100 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2200 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,2047,1993

 Safety Information

HS Code 2933499090

 Synthetic Route

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: US5011931 A1, ;

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , # 4 p. 387 - 392

~80%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Birch, Alan M.; Davies, Roy V.; Maclean, Lachlan; Robinson, Keith Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1994 , # 4 p. 387 - 392

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , # 4 p. 387 - 392

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , # 4 p. 387 - 392

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , # 4 p. 387 - 392

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , # 4 p. 387 - 392

~%

flosequinan Structure

flosequinan

CAS#:76568-02-0

Literature: Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , # 4 p. 387 - 392

 Customs

HS Code 2933499090
Summary 2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone
Manoplax
FLOSEQUINAN
7-Fluoro-1-methyl-3-(methylsulfinyl)quinolin-4(1H)-one
7-fluoro-1-methyl-3-methylsulfinyl-4-quinolone
[7-Fluoro-1-methyl-3-(methylsulfinyl)-4(1H)-quinolone]
4(1H)-Quinolinone,7-fluoro-1-methyl-3-(methylsulfinyl)
Flosequinan (USAN/INN)
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