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73080-51-0

73080-51-0 structure
73080-51-0 structure
  • Name: Repirinast
  • Chemical Name: 3-methylbutyl 7,8-dimethyl-4,5-dioxo-6H-pyrano[3,2-c]quinoline-2-carboxylate
  • CAS Number: 73080-51-0
  • Molecular Formula: C8H11N7O
  • Molecular Weight: 221.219
  • Catalog: API Respiratory medication Asthma
  • Create Date: 2018-08-19 11:12:15
  • Modify Date: 2024-01-02 13:23:27
  • Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma[1][2][3].
Name 3-methylbutyl 7,8-dimethyl-4,5-dioxo-6H-pyrano[3,2-c]quinoline-2-carboxylate
Synonyms Isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano(3,2-c)quinoline-2-carboxylate
MY-5116
Repirinastum [INN-Latin]
Diazenecarboxamide, 2-[4-[2-(diaminomethylene)hydrazinyl]phenyl]-, (E)-
Romet
Isopentyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano(3,2-c)quinoline-2-carboxylate
(E)-2-{4-[2-(Diaminomethylene)hydrazino]phenyl}diazenecarboxamide
repirinast
Description Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma[1][2][3].
Related Catalog
In Vitro Repirinast inhibits histamine release from rat peritoneal mast cells induced by antigen (IC50: 0.3 μM)[3].
In Vivo Repirinast (30 mg/kg, i.p.) inhibits antigen-induced early and late pulmonary responses in guinea pigs[1]. Repirinast (30 mg/kg, p.o.) inhibits antigen-induced immediate bronchoconstriction in rats[2]. Animal Model: Guinea pigs[1] Dosage: 30 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Inhibited leukocyte (predominantly eosinophils) infiltration into bronchial tissue. Blocked antigen-induced airway hyperresponsiveness to inhaled Acetylcholine. Animal Model: Rat with asthma (challenged with 10 mg/kg antigen OVA)[1] Dosage: 30 mg/kg Administration: Oral administration (p.o.) Result: Inhibited the decreases in the number Of breath at 30 sec and 1 min after challenge.
References

[1]. N Yamada, et al. Repirinast inhibits antigen-induced early and late pulmonary responses and airway hyperresponsiveness in guinea pigs. Int Arch Allergy Immunol. 1993;100(4):367-72.

[2]. Takahashi K. Effects of MY-5116 on experimental asthma in rats and guinea pigs. Arerugi. 1986 Oct; 35(10): 1037-46.

[3]. M Takei, et al. Inhibition of histamine release from rat peritoneal mast cells by MY-1250, an active metabolite of Repirinast (MY-5116). Int Arch Allergy Appl Immunol. 1990;93(2-3):237-41.

Density 1.6±0.1 g/cm3
Boiling Point 461.1±55.0 °C at 760 mmHg
Melting Point 236-241°
Molecular Formula C8H11N7O
Molecular Weight 221.219
Flash Point 232.6±31.5 °C
Exact Mass 221.102509
PSA 89.37000
LogP 0.46
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.731

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UQ1377000
CHEMICAL NAME :
4H-Pyrano(3,2-c)quinoline-2-carboxylic acid, 5,6-dihydro-7,8-dimethyl-4,5-dioxo-, isopentyl ester
CAS REGISTRY NUMBER :
73080-51-0
LAST UPDATED :
199612
DATA ITEMS CITED :
9
MOLECULAR FORMULA :
C20-H21-N-O5
MOLECULAR WEIGHT :
355.42

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 :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2783 mg/kg
TOXIC EFFECTS :
Gastrointestinal - peritonitis Kidney, Ureter, Bladder - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1435 mg/kg
TOXIC EFFECTS :
Gastrointestinal - peritonitis Kidney, Ureter, Bladder - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,577,1986
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Liver - other changes Kidney, Ureter, Bladder - changes primarily in glomeruli Blood - changes in spleen
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
5200 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Fertility - abortion Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,51,1986
HS Code 2934999090
63768-46-7 structure

63768-46-7

~%

73080-51-0 structure

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256
87-59-2 structure

87-59-2

~%

73080-51-0 structure

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256
63768-47-8 structure

63768-47-8

~%

73080-51-0 structure

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256
123-51-3 structure

123-51-3

73080-52-1 structure

73080-52-1

~%

73080-51-0 structure

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256
HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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