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Xipamide

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Chemical Structure| 14293-44-8 同义名 : -
CAS号 : 14293-44-8
货号 : A200352
分子式 : C15H15ClN2O4S
纯度 : 97%
分子量 : 354.809
MDL号 : MFCD00865927
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(704.61 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Xipamide is a sulfonamide-based diuretic. Xipamide is an antihypertensive agent able to selectively inhibit the anion exchanger (AE). The efficacy of xipamide 20 to 40 mg once daily in patients with mild to moderate hypertension is comparable to that of bendrofluazide 5 mg, bumetanide 1 mg or hydrochlorothiazide 50 mg when used alone in newly treated or previously treated patients[3]. 10 mg or 20 mg of xipamide daily is effective in lowering blood pressure in hypertensive patients but is associated with hypokalaemia[4]. The plasma concentration of alpha-atrial natriuretic peptide fell after 1 week of xipamide administration and increased during prolonged xipamide administration but remained reduced. The changes in plasma alpha-ANP observed after 1 week of xipamide were negatively correlated with the changes in hematocrit and hemoglobin. The xipamide-induced changes in PRA (Plasma renin activity) and PAC (aldosterone concentration) were positively correlated with the changes in the hematocrit and hemoglobin[5]. In newborn rat cardiomyocytes, xipamide reduced amiloride-induced cell acidification at similar concentrations as in H9c2 cardiocytes, but with a slightly higher extent of maximal inhibition (70-80%). Xipamide reduced amiloride-dependent cell acidification in the rat heart myogenic H9c2 cell line and in newborn rat cultured cardiomyocytes[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.82mL

0.56mL

0.28mL

14.09mL

2.82mL

1.41mL

28.18mL

5.64mL

2.82mL

参考文献

[1]Hempelmann FW. [Studies on Xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylidide). Part 1: Physico-chemical and chemical properties (author's transl)] . Arzneimittelforschung. 1977;27(11):2140-3. German.

[2]Weber JC, Bird H, et al. Once daily treatment of mild to moderate hypertension with xipamid: a controlled study. Br J Clin Pharmacol. 1977 Jun;4(3):283-8.

[3]Prichard BN, Brogden RN. Xipamide. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs. 1985 Oct;30(4):313-32

[4]MacGregor GA, Banks RA, Markandu ND, Roulston J. Xipamide and cyclopenthiazide in essential hypertension--comparative effects on blood pressure and plasma potassium. Br J Clin Pharmacol. 1982 Jun;13(6):859-63

[5]Lijnen P, Fagard R, Staessen J, Amery A. Hormonal effects of the diuretic xipamide in healthy men. Cardiovasc Drugs Ther. 1991 Aug;5(4):741-6

[6]Taouil K, Féray JC, Brunet J, Christen MO, Garay RP, Hannaert P. Inhibition by xipamide of amiloride-induced acidification in cultured rat cardiocytes. Eur J Pharmacol. 1997 Apr 18;324(2-3):289-94