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氯噻酮 |
| CAS No.: |
77-36-1 |
| 分子式： |
C14H11ClN2O4S |
| 分子量： |
338.77 |
| 备注： |
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)-benzenesulfonamidCAS号77-36-1分子式C14H11ClN2O4S分子量338.77EINECS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;医用原料;试剂盒-Elisa试剂盒;化学试剂;THALITONE;Amines;Heterocycles;Intermediates&FineChemicals;Pharmaceuticals;Sulfur&SeleniumCompounds;CHForensicandVeterinaryStandards;Alphabetic;C;Drugs&Metabolites;NeatCompoundsMol文件77-36-1.mol结构式氯塞酮性质熔点265-267°C(dec.)密度1.3356(roughestimate)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）形态粉末酸度系数(pKa)pKa9.4(Uncertain)颜色白色至米色水溶解性0.12g/L(25ºC)稳定性吸湿性InChIKeyJIVPVXMEBJLZRO-UHFFFAOYSA-NNIST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)氯塞酮用途与合成方法生物活性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Chlorthalidoneisathiazide-likediuretic.Afteroralintake,peakserumconcentrationsareachievedin2-6hours.Thehalf-lifeofChlorthalidoneisapproximately42(range29-55)hours,reaching45-60hoursafterlong-termdosing.However,inChemicalbookterindividualvariabilityinthehalf-lifeofChlorthalidoneiswide.Chlorthalidoneisexcretedunchangedbythekidneys.ThenatriureticeffectofChlorthalidoneismaximalat18hoursandlastsmorethan48hours.ComparingdifferentdosesofChlorthalidone,ithasbeenobservedthat25mgdailyisnearlyaseffectiveashigherdoses,butwithlessriskofhypokalemia.Chlorthalidonereducescalciumoxalatecalculousrecurrencebutmagnesiumhydroxidedoesnot.TheeffectivenessofChlorthalidoneormagnesiumhydroxideisexaminedinthepreventionofrecurrentcalciumoxalatekidneycalculi.Inadouble-blindrandomallocationdesigndailydosagesof25or50mg.Chlorthalidone,650or1,300mg.magnesiumhydroxide,oranidenticalplaceboareadministered.Allgroupsshowedsignificantlydecreasedcalculouseventscomparedtothepretreatmentrates.Duringthetrial56.1percentfewercalculithanpredicteddevelopedintheplacebogroup(plessthan0.01),whereasthegroupsreceivinglowandhighdosagemagnesiumhydroxideshowed73.9and62.3percentfewercalculi,respectively(plessthan0.001andlessthan0.01,respectively).Chlorthalidonetreatmentresultsina90.1percentdecreasefrompredictedratesandbothdosagesyieldedsimilarresults.WhenthetreatmentsarecomparedChlorthalidoneissignificantlybetterthantheplaceboormagnesiumhydroxide(plessthan0.01).Thelargedecreasesincalculouseventsseenwhenplaceboorineffectivetherapyisgivenunderscorethepositivetreatmentbiasthatoccurswhenhistoricalcontrolsareusedandtheydemonstratetheneedforproperexperimentaldesign.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。 |
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