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77-36-1

中文名称 氯塞酮
英文名称 Chlortalidone
CAS 77-36-1
分子式 C14H11ClN2O4S
分子量 338.77
MOL 文件 77-36-1.mol
更新日期 2024/05/29 11:25:11
77-36-1 结构式 77-36-1 结构式

基本信息

中文别名
氯塞酮
氯噻酮
氯塞酮(氯噻酮)
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/2-氯-5-(2,3-二氢-1-羟基-3-氧代-1H-异吲哚-1-基)苯磺酰胺
英文别名
renon
g33182
isoren
oradil
igroton
hygroton
hydroton
oxodolin
zambesil
NSC 6920
所属类别
原料药:利尿药

物理化学性质

外观性状白色结晶性粉末。熔点224-226℃(分解)。微溶于水、乙醇、氯仿,溶于热乙醇。无臭,无味。
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:可溶5mg/mL,澄清(加热)
酸度系数(pKa)pKa 9.4 (Uncertain)
形态粉末
颜色白色至米色
水溶解性0.12g/L(25 ºC)
稳定性吸湿性
InChIKeyJIVPVXMEBJLZRO-UHFFFAOYSA-N
NIST化学物质信息Chlorthalidone(77-36-1)

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H315-H319-H335
安全说明22-24/25
WGK Germany2
RTECS号DB1556000
海关编码2935904000
毒性LD50 oral in rabbit: > 5gm/kg

应用领域

用途1
利尿药,用于心脏性,肾性及其他水肿病。

制备方法

方法1
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。

常见问题列表

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.

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