氯塞酮
中文名称:
氯塞酮
中文同义词:
2-氯-5-(2,3-二氢-1-羟基-3-氧代-1H-异吲哚-1-基)苯磺酰胺;氯塞酮;氯噻酮溶液,100PPM;氯噻酮溶液,1000PPM;氯塞酮/2-氯-5-(2,3-二氢-1-羟基-3-氧代-1H-异吲哚-1-基)苯磺酰胺;氯塞酮(氯噻酮);氯吡酮杂质;氯噻酮
英文名称:
Chlortalidone
英文同义词:
thalitone;2-chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1h-isoindol-1-yl)benzenesulfonamide;hygroton;CHLORTHALIDONE;CHLORTALIDONE;1-keto-3-(3’-sulfamyl-4’-chlorophenyl)-3-hydroxyisoindoline;1-oxo-3-(3-sulfamyl-4-chlorophenyl)-3-hydroxyisoindoline;2-chloro-5-(1-hydroxy-3-oxo-1-isoindolinyl)-benzenesulfonamid
CAS号:
77-36-1
分子式:
C14H11ClN2O4S
分子量:
338.77
EINECS号:
201-022-5
相关类别:
原料药;小分子抑制剂;无机化合物和盐;有机化学;有机中间体;医药原料药-科研原料;农药原料;原料;THALITONE;Amines;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;Sulfur Selenium Compounds;CHForensic and Veterinary Standards;Alphabetic;C;DrugsMetabolites;Neat Compounds
Mol文件:
77-36-1.mol
熔点
265-267°C (dec.)
密度
1.3356 (rough estimate)
折射率
1.5630 (estimate)
储存条件
2-8°C
溶解度
DMSO: soluble5mg/mL, clear (warmed)
形态
powder
酸度系数(pKa)
pKa 9.4 (Uncertain)
颜色
white to beige
水溶解性
0.12g/L(25 ºC)
InChIKey
JIVPVXMEBJLZRO-UHFFFAOYSA-N
NIST化学物质信息
Chlorthalidone(77-36-1)
EPA化学物质信息
Benzenesulfonamide, 2-chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1H-isoindol-1-yl)- (77-36-1)
生物活性
Chlortalidone (Chlortalidone)是一种利尿剂，用于治疗高血压。
体外研究
Chlorthalidone通过抑制钠离子通过肾小管上皮细胞的转运，增加钠，氯，和水排泄到肾内腔。它作用的主要位点是髓袢上升支的皮质稀释段。通过增加钠到远端肾小管的转运，chlorthalidone通过钠钾交换机制间接增加钾分泌(即顶端ROMK/Na 通道耦合基底侧NKATPases)。
体内研究
Chlorthalidone is a thiazide-like diuretic. After oral intake, peak serum concentrations are achieved in 2-6 hours. The half-life of Chlorthalidone is approximately 42 (range 29-55) hours, reaching 45-60 hours after long-term dosing. However, interindividual variability in the half-life of Chlorthalidone is wide. Chlorthalidone is excreted unchanged by the kidneys. The natriuretic effect of Chlorthalidone is maximal at 18 hours and lasts more than 48 hours. Comparing different doses of Chlorthalidone, it has been observed that 25 mg daily is nearly as effective as higher doses, but with less risk of hypokalemia. Chlorthalidone reduces calcium oxalate calculous recurrence but magnesium hydroxide does not. The effectiveness of Chlorthalidone or magnesium hydroxide is examined in the prevention of recurrent calcium oxalate kidney calculi. In a double-blind random allocation design daily dosages of 25 or 50 mg. Chlorthalidone, 650 or 1,300 mg. magnesium hydroxide, or an identical placebo are administered. All groups showed significantly decreased calculous events compared to the pretreatment rates. During the trial 56.1 per cent fewer calculi than predicted developed in the placebo group (p less than 0.01), whereas the groups receiving low and high dosage magnesium hydroxide showed 73.9 and 62.3 per cent fewer calculi, respectively (p less than 0.001 and less than 0.01, respectively). Chlorthalidone treatment results in a 90.1 per cent decrease from predicted rates and both dosages yielded similar results. When the treatments are compared Chlorthalidone is significantly better than the placebo or magnesium hydroxide (p less than 0.01). The large decreases in calculous events seen when placebo or ineffective therapy is given underscore the positive treatment bias that occurs when historical controls are used and they demonstrate the need for proper experimental design.
化学性质
白色结晶性粉末。熔点224-226℃（分解）。微溶于水、乙醇、氯仿，溶于热乙醇。无臭，无味。
用途
利尿药，用于心脏性，肾性及其他水肿病。
生产方法
由2-（3-氨基-4-氯苯甲酰）苯甲酸[118-04-7]经重氮化、置换、氯磺化、环合、胺化而得。
安全说明
22-24/25
WGK Germany
2
RTECS号
DB1556000
海关编码
2935904000
毒害物质数据
77-36-1(Hazardous Substances Data)
毒性
LD50 oral in rabbit: > 5gm/kg
