123040-16-4

中文名称盐酸阿扎司琼

英文名称 Azasetron hydrochloride

CAS 123040-16-4

分子式 C17H21Cl2N3O3

MDL 编号 MFCD00209913

分子量 386.27

MOL 文件 123040-16-4.mol

更新日期 2024/05/11 12:50:17

123040-16-4 结构式

基本信息物理化学性质安全数据应用领域常见问题列表

基本信息

中文别名

盐酸阿扎司琼
N-(1-氮杂双环[2.2.2]辛-8-基)-6-氯-4-甲基-3-氧代-3,4-二氢-2H-1,4-苯并恶嗪-8-甲酰胺盐酸盐
盐酸阿扎司琼

英文别名

AZASETRON
AZASETRON HCL
AZASETRON 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, HYDROCHLORIDE
N-(1-AZABICYCLO[2.2.2]OCT-3-YL)-6-CHLORO-4-METHYL-3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZINE-8-CARBOXAMIDE HCL
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
Y-25130
Y-25130 HYDROCHLORIDE
2h-1,4-benzoxazine-8-carboxamide,3,4-dihydro-n-1-azabicyclo(2.2.2)oct-3-yl-6-c
N-(1-Azabicyclo[2,2,2]Oct-3-Yl)-6-Chloro-4-Methyl-3-Oxo-3,4-Dihydro-2h-1,4-Benzoxazine-8-Carboxamide HCl
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
Y-25130HCl
N-(1-Azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzo
INTERMEDIATE OF AZASETRON HCL
Serotone
Azasetron hydrochloride
N-(1-Azabicyclo[2.2.2]octan-8-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide hydrochloride
N-(1-Azabicyclo[2.2.2]octane-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide·hydrochloride

所属类别

原料药：止吐催吐药

物理化学性质

外观白色粉末。

熔点281° (dec); mp 305° (dec) (Kawakita)

储存条件Sealed in dry,Room Temperature

溶解度甲醇（微溶）、水（微溶）

溶解度少许溶于甲醇和水

形态白色固体。

颜色白色

CAS 数据库123040-16-4(CAS DataBase Reference)

贮存方式-20℃低温保存.

原研厂家Japan Tobacco (Originator), Mitsubishi Pharma (Originator), Taiho (Not Determined), Torii (Marketer), Temis-Lostalo (Licensee).

安全数据

危险性符号(GHS)

GHS08

警示词警告

危险性描述H361

防范说明P201-P202-P281-P308+P313-P405-P501

毒性LD50 in male, female rats (mg/kg): 135, 132 i.v. (Takagi)

应用领域

用途一

盐酸阿扎司琼【123040-16-4】是抗生素类抗感染原料药，用于细胞毒类药物引起的恶心、呕吐。用于放疗引起的恶心、呕吐。用于妇科手术及外科手术引起的恶心、呕吐。

常见问题列表

生物活性

Azasetron HCl (Y-25130) 是一种选择性5-HT3受体拮抗剂，IC50为0.33 nM，用于癌症化疗引起的恶心和呕吐。

靶点

Target	Value
5-HT3	0.33 nM

体内研究

Azasetron could effectively penetrate through the skin and pass into the systemic circulation.

Animal Model:	Four male Bama miniature pigs weighing 9-11 kg (15-16 weeks old).
Dosage:	0.5 mg/kg.
Administration:	I.V. administration via the abdominal vein.
Result:	The mean plasma concentration dropped to minimum at 36 h. C _max = 44.88 ± 7.16 ng/mL) was achieved at the time point of 66.00 ± 22.98 h (T _max ).