乙吗噻嗪
中文名称 | 乙吗噻嗪 |
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中文同义词 | 莫瑞西嗪;10-(3-吗啉基丙酰基)吩噻嗪-2-氨基甲酸乙酯;安脉静;安他脉静;吗拉西嗪;乙吗噻嗪;盐酸莫雷西嗪;化合物 T16127 |
英文名称 | Moricizine |
英文同义词 | TIMTEC-BB SBB005991;CARBAMIC ACID, [10-[3-(4-MORPHOLINYL)-1-OXOPROPYL]-10H-PHENOTHIAZIN-2-YL]-, ETHYL ESTER;Moricizine;Moricizin;10-(3-Morpholinopropionyl)-10H-phenothiazin-2-yl carbaminoic acid, ethyl ester;10-(3-Morpholinopropionyl)phenothiazine-2-carbamic acid ethyl ester;Ethmozin:Moricizine;N-[10-(3-Morpholinopropionyl)-10H-phenothiazin-2-yl]carbamic acid ethyl ester |
CAS号 | 31883-05-3 |
分子式 | C22H25N3O4S |
分子量 | 427.52 |
EINECS号 | 250-854-5 |
相关类别 | 抗心律失常药;心脑血管药物;药物;生物化工;API |
Mol文件 | 31883-05-3.mol |
结构式 |
乙吗噻嗪 性质
熔点 | 156-157° |
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沸点 | 625.0±55.0 °C(Predicted) |
密度 | 1.315±0.06 g/cm3(Predicted) |
储存条件 | -20°C Freezer, Under inert atmosphere |
溶解度 | 可溶于氯仿(轻微)、甲醇(非常轻微) |
酸度系数(pKa) | 6.4(at 25℃) |
形态 | 固体 |
颜色 | 浅橙色到浅橙色 |
Moricizine (Moracizine) induces the tonic block of INa with the apparent dissociation constant (Kd,app) of 6.3 microM at -100 mV and 99.3 microM at -140 mV. Moricizine at 30 microM shifts the h infinity curve to the hyperpolarizing direction by 8.6 +/- 2.4 mV. Moricizine also produces the phasic block of INa, which is enhanced with the increase in the duration of train pulses, and is more prominent with a holding potential (HP) of -100 mV than with an HP of -140 mV. Moricizine exerts an antiarrhythmic action on atrial myocytes, as well as on ventricular myocytes, by blocking Na+ channels with a high affinity to the inactivated state and a slow dissociation kinetics.
盐酸莫雷西嗪(Moracizine Hydrochloride):C22H25N3O4S?HCl。[29560-58-5]。从二氯乙烷得白色结晶。溶于水或醇。熔点189"C(分解)。急性毒性LD50小鼠,大鼠(mg/kg):36,12静脉注射。急性毒性LD50小鼠(mg/kg):131腹腔注射。
10.2g上面得到的酯化合物溶于50ml甲苯,加入4.72g吗啉,在110~120℃回流3h。过滤除去沉淀出的吗啉盐酸盐,滤液用水洗以除去过剩的吗啉,然后用稀盐酸酸化至Ph值为3。分出酸性水层,用活性炭处理后,再碱化至Ph值为8-9。即得莫雷西嗪,熔点156-157℃。
上面得到的莫雷西嗪用甲苯萃取,萃取液用无水硫酸镁干燥。往该无水甲苯溶液中,加入氯化氢的无水乙醚溶液,直至盐酸莫瑞西嗪完全沉淀出来。该沉淀用二氯甲烷重结晶,得9.35g盐酸莫雷西嗪,收率76.2%,熔点189℃(分解)。