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77-36-1

中文名稱 氯塞酮
英文名稱 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 2024/12/22 16:32:13
77-36-1 結(jié)構(gòu)式 77-36-1 結(jié)構(gòu)式

基本信息

中文別名
氯塞酮
氯噻酮
氯塞酮(氯噻酮)
2-氯-5-(2,3-二氫-1-羥基-3-氧代-1H-異吲哚-1-基)苯磺酰胺
氯塞酮/2-氯-5-(2,3-二氫-1-羥基-3-氧代-1H-異吲哚-1-基)苯磺酰胺
英文別名
renon
g33182
isoren
oradil
igroton
hygroton
hydroton
oxodolin
zambesil
NSC 6920
所屬類別
原料藥:利尿藥

物理化學性質(zhì)

外觀性狀白色結(jié)晶性粉末。熔點224-226℃(分解)。微溶于水、乙醇、氯仿,溶于熱乙醇。無臭,無味。
熔點265-267°C (dec.)
密度1.3356 (rough estimate)
折射率1.5630 (estimate)
儲存條件2-8°C
溶解度DMSO:可溶5mg/mL,澄清(加熱)
酸度系數(shù)(pKa)pKa 9.4 (Uncertain)
形態(tài)粉末
顏色白色至米色
水溶解性0.12g/L(25 ºC)
穩(wěn)定性吸濕性
InChIKeyJIVPVXMEBJLZRO-UHFFFAOYSA-N
NIST化學物質(zhì)信息Chlorthalidone(77-36-1)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
安全說明22-24/25
WGK Germany2
RTECS號DB1556000
海關(guān)編碼2935904000
毒害物質(zhì)數(shù)據(jù)77-36-1(Hazardous Substances Data)
毒性LD50 oral in rabbit: > 5gm/kg

應(yīng)用領(lǐng)域

用途1
利尿藥,用于心臟性,腎性及其他水腫病。

制備方法

方法1
由2-(3-氨基-4-氯苯甲酰)苯甲酸[118-04-7]經(jīng)重氮化、置換、氯磺化、環(huán)合、胺化而得。
氯塞酮價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/11XW00773611氯塞酮77-36-150MG49元
2024/11/0846093氯噻酮
Chlorthalidone, 98%, Thermo Scientific Chemicals
77-36-1250mg588元
2024/11/0846093氯噻酮
Chlorthalidone, 98%, Thermo Scientific Chemicals
77-36-11g1715元

常見問題列表

生物活性
Chlortalidone (Chlortalidone)是一種利尿劑,用于治療高血壓。
體外研究

Chlorthalidone通過抑制鈉離子通過腎小管上皮細胞的轉(zhuǎn)運,增加鈉,氯,和水排泄到腎內(nèi)腔。它作用的主要位點是髓袢上升支的皮質(zhì)稀釋段。通過增加鈉到遠端腎小管的轉(zhuǎn)運,chlorthalidone通過鈉鉀交換機制間接增加鉀分泌(即頂端ROMK/Na 通道耦合基底側(cè)NKATPases)。

體內(nèi)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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