吉非罗齐杂质A结构式
|
常用名 | 吉非罗齐杂质A | 英文名 | proguanil hydrochloride |
|---|---|---|---|---|
| CAS号 | 637-32-1 | 分子量 | 290.192 | |
| 密度 | N/A | 沸点 | 402.7ºC at 760 mmHg | |
| 分子式 | C11H17Cl2N5 | 熔点 | 249-251ºC | |
| MSDS | 中文版 美版 | 闪点 | 197.4ºC | |
| 符号 |
GHS06 |
信号词 | Danger |
吉非罗齐杂质A用途Proguanil hydrochloride是一种抗疟前药,被代谢为活性代谢物环鸟苷 (HY-12784)。Proguanil hydrochloride是一种二氢叶酸还原酶 (DHFR) 抑制剂。 |
| 中文名 | 吉非罗齐杂质A |
|---|---|
| 英文名 | Proguanil hydrochloride |
| 中文别名 | 盐酸氯胍 |
| 英文别名 | 更多 |
| 描述 | Proguanil hydrochloride是一种抗疟前药,被代谢为活性代谢物环鸟苷 (HY-12784)。Proguanil hydrochloride是一种二氢叶酸还原酶 (DHFR) 抑制剂。 |
|---|---|
| 相关类别 | |
| 体外研究 | 丙胍本身体外抗疟活性较弱(IC50=2.4-19μM),其有效性取决于活性代谢物环鸟苷(IC50=0.5-2.5nm)。环鸟苷是一种二氢叶酸还原酶(DHFR)抑制剂。阿托瓦醌与普罗瓜尼的联合作用在体外具有协同作用。这两种药物还具有抗疟原虫配子体和红细胞前(肝)阶段的活性[1]。丙胍作为双胍而不是其代谢物环鸟苷(一种寄生虫二氢叶酸还原酶[DHFR]抑制剂)来增强阿托伐酮效应。丙胍介导的增强作用对阿托瓦醌是特异性的,因为其他线粒体电子传递抑制剂(如粘噻唑和抗霉素)的作用不会因包合丙胍而改变[2]。5-HT3受体反应可被丙胍、代谢物4-氯苯基-1-双胍(CPB)和活性代谢物环鸟苷(CG)可逆抑制,IC50分别为1.81、1.48和4.36μM[3]。 |
| 体内研究 | 普罗胍(p.o.；2.9mg/kg体重；每日5天和6周)在wistar系白化大鼠中表现出轻微的退行性变化,而在6周内表现出严重的退行性变化[4]。普罗古尼治疗组大鼠血清睾酮水平显著降低[4]。给实验性感染吉布森B.gibsoni的2只狗在慢性期和3只急性期使用马拉酮(阿托瓦醌和普罗古尼)可减少寄生虫血症,并观察到临床改善[5]。 |
| 参考文献 |
| 沸点 | 402.7ºC at 760 mmHg |
|---|---|
| 熔点 | 249-251ºC |
| 分子式 | C11H17Cl2N5 |
| 分子量 | 290.192 |
| 闪点 | 197.4ºC |
| 精确质量 | 289.086090 |
| PSA | 83.79000 |
| LogP | 4.06530 |
| 储存条件 | -20°C Freezer |
| 水溶解性 | acetonitrile: water: ~1mg/mL (60/40) |
|
CYP2C19*17 increases clopidogrel-mediated platelet inhibition but does not alter the pharmacokinetics of the active metabolite of clopidogrel.
Clin. Exp. Pharmacol. Physiol. 41(11) , 870-8, (2014) The aim of the present study was to determine the impact of CYP2C19*17 on the pharmacokinetics and pharmacodynamics of the active metabolite of clopidogrel and the pharmacokinetics of proguanil. Thus,... |
|
|
The antimalarial drug proguanil is an antagonist at 5-HT3 receptors.
J. Pharmacol. Exp. Ther. 351(3) , 674-84, (2014) Proguanil is an antimalarial prodrug that is metabolized to 4-chlorophenyl-1-biguanide (CPB) and the active metabolite cycloguanil (CG). These compounds are structurally related to meta-chlorophenyl b... |
|
|
Paper test cards for presumptive testing of very low quality antimalarial medications.
Am. J. Trop. Med. Hyg. 92 , 17-23, (2015) Carrying out chemical analysis of antimalarials to detect low-quality medications before they reach a patient is a costly venture. Here, we show that a library of chemical color tests embedded on a pa... |
| Imidodicarbonimidic diamide, N-(4-chlorophenyl)-N'-(1-methylethyl)-, monohydrochloride |
| Biguanide, 1- (p-chlorophenyl)-5-isopropyl-, monohydrochloride |
| N-(4-chlorophenyl)-N'-(1-methylethyl)imidodicarbonimidic diamide hydrochloride |
| diamide N-(4-chlorophényl)-N'-(1-méthyléthyl)imidodicarbonimidique chlorhydrate |
| Paludrin |
| proguanil hydrochloride |
| Paludrine |
| N-(4-Chlorophenyl)-N'-isopropylimidodicarbonimidic diamide hydrochloride (1:1) |
| Drinupal hydrochloride |
| Tirian hydrochloride |
| Palusil hydrochloride |
| Imidodicarbonimidic diamide, N-(4-chlorophenyl)-N'-(1-methylethyl)-, hydrochloride (1:1) |
| N-(4-chlorophenyl)-N'-propan-2-ylimidodicarbonimidic diamide hydrochloride (1:1) |
| N-(4-Chlorphenyl)-N'-(1-methylethyl)imidodicarbonimidic diamidhydrochlorid |
