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氯噻酮 |
| CAS No.: |
77-36-1 |
| 分子式： |
C14H11ClN2O4S |
| 分子量： |
338.77 |
| 備注： |
中文名稱氯塞酮中文同義詞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;氯噻酮溶液,100PPM;氯噻酮溶液,1000PPM;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;氯塞酮(氯噻酮);氯吡酮雜質;氯噻酮英文名稱Chlortalidone英文同義詞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號77-36-1分子式C14H11ClN2O4S分子量338.77EINECS號201-022-5相關類別原料藥;小分子抑制劑;無機化合物和鹽;有機化學;有機中間體;醫(yī)藥原料藥-科研原料;農藥原料;原料;醫(yī)用原料;試劑盒-Elisa試劑盒;化學試劑;THALITONE;Amines;Heterocycles;Intermediates&FineChemicals;Pharmaceuticals;Sulfur&SeleniumCompounds;CHForensicandVeterinaryStandards;Alphabetic;C;Drugs&Metabolites;NeatCompoundsMol文件77-36-1.mol結構式氯塞酮性質熔點265-267°C(dec.)密度1.3356(roughestimate)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）形態(tài)粉末酸度系數(pKa)pKa9.4(Uncertain)顏色白色至米色水溶解性0.12g/L(25oC)穩(wěn)定性吸濕性InChIKeyJIVPVXMEBJLZRO-UHFFFAOYSA-NNIST化學物質信息Chlorthalidone(77-36-1)EPA化學物質信息Benzenesulfonamide,2-chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1H-isoindol-1-yl)-(77-36-1)氯塞酮用途與合成方法生物活性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運，增加鈉，氯，和水排泄到腎內腔。它作用的主要位點是髓袢上升支的皮質稀釋段。通過增加鈉到遠端腎小管的轉運，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NKATPases)。體內研究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.化學性質白色結晶性粉末。熔點224-226℃（分解）。微溶于水、乙醇、氯仿，溶于熱乙醇。無臭，無味。用途利尿藥，用于心臟性，腎性及其他水腫病。生產方法由2-（3-氨基-4-氯苯甲酰）苯甲酸[118-04-7]經重氮化、置換、氯磺化、環(huán)合、胺化而得。 |
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