中文名 | 氯噻酮 |
英文名 | Chlorthalidone |
别名 | 氯噻酮 氯塞酮 氯吡酮杂质 氯塞酮(氯噻酮) 氯噻酮溶液,100PPM 氯噻酮溶液,1000PPM 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 | hygroton thalitone CHLORTALIDONE Chlortalidone CHLORTHALIDONE Chlorthalidone 1-oxo-3-(3-sulfamyl-4-chlorophenyl)-3-hydroxyisoindoline 3-(4-chloro-3-sulphamoylphenyl)-3-hydroxyisoindolin-1-one 1-keto-3-(3'-sulfamyl-4'-chlorophenyl)-3-hydroxyisoindoline 2-chloro-5-(1-hydroxy-3-oxo-1-isoindolinyl)-benzenesulfonamid 2-chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzenesulfonamide 2-chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1h-isoindol-1-yl)benzenesulfonamide |
CAS | 77-36-1 |
EINECS | 201-022-5 |
化学式 | C14H11ClN2O4S |
分子量 | 338.77 |
InChI | InChI=1/C14H11ClN2O4S/c15-11-6-5-8(7-12(11)22(16,20)21)14(19)10-4-2-1-3-9(10)13(18)17-14/h1-7,19H,(H,17,18)(H2,16,20,21) |
InChIKey | JIVPVXMEBJLZRO-UHFFFAOYSA-N |
密度 | 1.3356 (rough estimate) |
熔点 | 265-267°C (dec.) |
水溶性 | 0.12g/L(25 ºC) |
溶解度 | DMSO: 可溶5mg/mL,澄清 (温热) |
折射率 | 1.5630 (estimate) |
酸度系数 | pKa 9.4 (Uncertain) |
存储条件 | 2-8°C |
稳定性 | 吸湿性 |
外观 | 粉末 |
颜色 | white to beige |
物化性质 | 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。 |
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. |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 2 |
RTECS | DB1556000 |
海关编号 | 2935904000 |
上游原料 | 2-(3-氨基-4-氯苯甲酰)苯甲酸 氨 氯化亚砜 盐酸 二氧化硫 |
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