鹽酸阿扎司瓊
| 中文名稱 | 鹽酸阿扎司瓊 |
|---|---|
| 中文同義詞 | N-(1-氮雜雙環(huán)[2.2.2]辛-8-基)-6-氯-4-甲基-3-氧代-3,4-二氫-2H-1,4-苯并惡嗪-8-甲酰胺鹽酸鹽;鹽酸阿扎司瓊;半合成脂肪酸甘油酯 (又名混合脂肪酸甘油酯);半混甘脂;鹽酸阿扎西隆;6-氯-4-甲基-3-氧代-N-(奎寧環(huán)-3-基)-3,4-二氫-2H-苯并[B][1,4]惡嗪-8-甲酰胺鹽酸鹽 |
| 英文名稱 | Azasetron hydrochloride |
| 英文同義詞 | 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;6-chloro-3-keto-4-methyl-N-quinuclidin-3-yl-1,4-benzoxazine-8-carboxamide hydrochloride;N-{1-azabicyclo[2.2.2]octan-3-yl}-6-chloro-4-Methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxaMide;Azastron hydrochloride injection;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);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 |
| CAS號 | 123040-16-4 |
| 分子式 | C17H21Cl2N3O3 |
| 分子量 | 386.27 |
| EINECS號 | 692-159-3 |
| 相關(guān)類別 | 小分子抑制劑;有機原料;止吐藥物;神經(jīng)信號;標(biāo)準(zhǔn)品;中藥對照品;醫(yī)藥原料和中間體;anti-emetic;Serotonin receptor;醫(yī)藥、農(nóng)藥及染料中間體;化工原料 |
| Mol文件 | 123040-16-4.mol |
| 結(jié)構(gòu)式 |  |
鹽酸阿扎司瓊 性質(zhì)
| 熔點 | 281° (dec); mp 305° (dec) (Kawakita) |
|---|---|
| 儲存條件 | Sealed in dry,Room Temperature |
| 溶解度 | 甲醇（微溶）、水（微溶） |
| 形態(tài) | 白色固體。 |
| 顏色 | 白色 |
| 水溶解性 | H2O: 2mg/mL, clear |
| CAS 數(shù)據(jù)庫 | 123040-16-4(CAS DataBase Reference) |
Azasetron HCl (Y-25130) 是一種選擇性5-HT3受體拮抗劑，IC50為0.33 nM，用于癌癥化療引起的惡心和嘔吐。
| Target | Value |
| 5-HT3 | 0.33 nM |
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 ). |
用途
預(yù)防化療引起的惡心嘔吐（5-HT3受體拮抗劑）安全信息
| 毒性 | LD50 in male, female rats (mg/kg): 135, 132 i.v. (Takagi) |
|---|
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2024/11/08 | 46507 | 鹽酸阿扎司瓊 Azasetron hydrochloride | 123040-16-4 | 250mg | 3188元 |
| 2024/11/08 | 46507 | 鹽酸阿扎司瓊 Azasetron hydrochloride | 123040-16-4 | 1g | 8839元 |