Azasetron HCl

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

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].

Name	Azasetron hydrochloride
Synonym	More Synonyms

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	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
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.

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Neurological Disease

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.

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

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 Phrases	S22-S24/25
WGK Germany	3

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

CAS#:76883-48-2

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

CAS#:123040-50-6

Azasetron HCl

CAS#:123040-16-4

Literature: US4892872 A1, ;

Precursor 2
CAS#:76883-48-2 (RS)-3-amino-1-... CAS#:123040-50-6 6-CHLORO-3,4-DI...
DownStream 0

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

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China
Product Name: Azasetron HCl
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Purity: 98.0%
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DC Chemicals Limited
China
Product Name: Azasetron HCL
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Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Azasetron hydrochloride
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Purity: 98.0%
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Zhejiang Hangyu API Co., Ltd
China
Product Name: Azasetron hydrochloride
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

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Azasetron HCl

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