Azasetron HCl

Modify Date: 2024-01-06 17:14:19

Azasetron HCl Structure
Azasetron HCl structure
 Common Name Azasetron HCl
CAS Number 123040-16-4 Molecular Weight 386.273
Density N/A Boiling Point 558ºC at 760 mmHg
Molecular Formula C17H21Cl2N3O3 Melting Point N/A
MSDS N/A Flash Point 291.2ºC

 Use of Azasetron HCl


Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. Target: 5-HT3 ReceptorAzasetron Hydrochloride is a 5-HT3 receptor antagonist which is used as an anti-emetic.Azasetron inhibited the specific binding of [3H]quipazine to 5-HT3 receptors at the synaptic membranes of the rat cerebral cortex with a Ki value of 2.9 nM. Azasetron showed low affinity for histamine H1 receptors (IC50 = 4.4 microM) but it could not reveal any affinities for the other receptors (5-HT1A, 5-HT2, dopamine D1, dopamine D2, alpha 1-adrenoceptor, alpha 2-adrenoceptor, muscarine and benzodiazepine) even at a 10 microM concentration [1]. Azasetron (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. Azasetron is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone [2].

 Names

Name Azasetron hydrochloride
Synonym More Synonyms

 Azasetron HCl Biological Activity

Description Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. Target: 5-HT3 ReceptorAzasetron Hydrochloride is a 5-HT3 receptor antagonist which is used as an anti-emetic.Azasetron inhibited the specific binding of [3H]quipazine to 5-HT3 receptors at the synaptic membranes of the rat cerebral cortex with a Ki value of 2.9 nM. Azasetron showed low affinity for histamine H1 receptors (IC50 = 4.4 microM) but it could not reveal any affinities for the other receptors (5-HT1A, 5-HT2, dopamine D1, dopamine D2, alpha 1-adrenoceptor, alpha 2-adrenoceptor, muscarine and benzodiazepine) even at a 10 microM concentration [1]. Azasetron (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. Azasetron is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone [2].
Related Catalog
References

[1]. Sato, N., et al., Antagonistic activity of Y-25130 on 5-HT3 receptors. Jpn J Pharmacol, 1992. 59(4): p. 443-8.

[2]. Haga, K., et al., The effects of orally administered Y-25130, a selective serotonin3-receptor antagonist, on chemotherapeutic agent-induced emesis. Jpn J Pharmacol, 1993. 63(3): p. 377-83.

 Chemical & Physical Properties

Boiling Point 558ºC at 760 mmHg
Molecular Formula C17H21Cl2N3O3
Molecular Weight 386.273
Flash Point 291.2ºC
Exact Mass 385.096008
PSA 61.88000
LogP 2.71500
Storage condition Desiccate at -20°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DM3001200
CHEMICAL NAME :
2H-1,4-Benzoxazine-8-carboxamide, 3,4-dihydro-N-1-azabicyclo(2.2.2)oct-3-yl-6-chloro-4- methyl-3-oxo-, monohydrochloride
CAS REGISTRY NUMBER :
123040-16-4
LAST UPDATED :
199706
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C17-H20-Cl-N3-O3.Cl-H
MOLECULAR WEIGHT :
386.31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
132 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,255,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,7,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
910 mg/kg/13W-I
TOXIC EFFECTS :
Behavioral - food intake (animal) Endocrine - changes in spleen weight Nutritional and Gross Metabolic - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,255,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
9100 mg/kg/13W-I
TOXIC EFFECTS :
Behavioral - ataxia Gastrointestinal - nausea or vomiting Blood - changes in bone marrow (not otherwise specified)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 51,343,1996
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
2730 mg/kg/91D-I
TOXIC EFFECTS :
Liver - other changes Endocrine - hypoglycemia Blood - pigmented or nucleated red blood cells
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 43,489,1992 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
7500 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception female 20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other 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 :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 52,77,1996
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
1100 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - physical
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 44,61,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
2600 mg/kg
SEX/DURATION :
female 7-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - physical
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 44,79,1992

 Safety Information

Safety Phrases S22-S24/25
WGK Germany 3

 Synthetic Route

(RS)-3-amino-1-azabicyclo[2.2.2]octane structure

(RS)-3-amino-1-...

CAS#:76883-48-2

6-CHLORO-3,4-DIHYROGEN-4-METHYL-3-OXO-2H-1,4-BENZOXAZOLE-8-ACYLCHLORIDE structure

6-CHLORO-3,4-DI...

CAS#:123040-50-6

~%

Azasetron HCl Structure

Azasetron HCl

CAS#:123040-16-4

Literature: US4892872 A1, ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Synonyms

Azasetron HCl
UNII:2BSS7XL60S
AZASETRON
Azasetron (hydrochloride)
MFCD00209913
Y-25130 Hydrochloride
N-1-AZABICYCLO[2.2.2]OCT-3-YL-6-CHLORO-3,4-DIHYDRO-4-METHYL-3-OXO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE
Serotone
2H-1,4-BENZOXAZINE-8-CARBOXAMIDE,N-1-AZABICYCLO[2.2.2]OCT-3-YL-6-CHLORO-3,4-DIHYDRO-4-METHYL-3-OXO-,HYDROCHLORIDE (1:1)
N-(1-Azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide hydrochloride (1:1)
INTERMEDIATE OF AZASETRON HCL
2H-1,4-BENZOXAZINE-8-CARBOXAMIDE, 3,4-DIHYDRO-N-1-AZABICYCLO(2.2.2)OCT-3-YL-6-C
Azasetron hydrochloride
2H-1,4-Benzoxazine-8-carboxamide, N-1-azabicyclo[2.2.2]oct-3-yl-6-chloro-3,4-dihydro-4-methyl-3-oxo-, hydrochloride (1:1)
N-(1-AZABICYCLO[2.2.2]OCT-3-YL)-6-CHLORO-4-METHYL-3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE HYDROCHLORIDE
Azasetronhydrochloride
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.
Top Suppliers:I want be here

Get all suppliers and price by the below link:

Azasetron HCl suppliers

Price: ￥444.6/10mg

Reference only. check more Azasetron HCl price

Related Compounds: More...
Azasetron HCl
123040-69-7
azasetron
123040-93-7
Azasetron hydrochloride
141922-90-9
Azasetron
123040-95-9
EPZ020411 HCl
1700663-41-7
Difelikefalin HCl
2711717-77-8
MDL72274 HCl
85278-24-6
Carbomethoxyformamidine HCl
60189-97-1
Meclizine HCl
31884-77-2
2-(4-Bromo-1H-pyrazol-1-yl)cyclobutan-1-one
2432829-50-8
4-Bromo-1-(2,2-dimethoxycyclobutyl)-1H-pyrazole
2433768-39-7
Rel-(1s,3s)-3-(4-bromo-1H-pyrazol-1-yl)-1-methylcyclobutan-1-ol
2432829-49-5
(4-bromo-1-tert-butyl-5-methyl-1H-pyrazol-3-yl)methanol
2138340-99-3
4-Bromo-5-(difluoromethyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole
2432829-41-7
1-Amino-5-bromo-3-methyl-6-oxo-pyridine-2-carboxamide
2423908-46-5
1,1-Dimethylethyl 4-[2-(5-chloro-2-pyridinyl)-2-methyl-1,3-benzodioxol-4-yl]-1-piperidinecarboxylate
2401894-21-9
1,3,5-Tris((3-methylpyridin-2-yl)oxy)benzene
2389235-12-3
4-chloro-6-methoxy-7-nitroQuinoline
2518371-70-3
N-(5-Bromopyridin-3-yl)tetrahydro-2H-pyran-4-carboxamide
1875689-46-5
Chemsrc provides Azasetron HCl(CAS#:123040-16-4) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Azasetron HCl are included as well.>> amp version: Azasetron HCl

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved