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Hydralazine HCl

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Chemical Structure| 304-20-1 同义名 : 1-肼苯哒嗪盐酸盐 ;Hydralazine (hydrochloride);1-Hydrazinophthalazine;Nepresol;mono-Hydrochloride, Hydralazine;Hydralazine chloride;Apresoline;Aiselazine;1-Hydrazinophthalazine hydrochloride;Hydralazine hydrochloride
CAS号 : 304-20-1
货号 : A256420
分子式 : C8H9ClN4
纯度 : 98%
分子量 : 196.637
MDL号 : MFCD00135998
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(127.14 mM)，配合低频超声，并调节pH至11，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

H2O: 25 mg/mL(127.14 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 31 mg/mL suspension

生物活性
描述 Hydralazine hydrochloride (HHC) is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles. The preliminary IV administration of dihydralazine allowed a reduced volatile agent concentration which attenuated undesirable haemodynamic effects, in spite of renin and norepinephrine release, and permitted a rapid intraoperative awakening[3]. Hydralazine hydrochloride may reduce blood pressure when compared to placebo in patients with primary hypertension, however this data is based on before and after studies, not RCTs (randomized controlled trials)[4]. The suitability of the prepared HHC sublingual tablets for use in rapid control on hypertensive crisis especially in pregnant women as an alternate to parenteral administration[5]. The combination consists of 20 mg of isosorbide and 37.5 mg hydralazine hydrochloride in a fixed dose that functions as a nitric oxide enhancer and an antioxidant, and helps to prevent tolerance to the prolonged use of nitrate[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02884011 - Completed - United States, Illinois ... 展开 >> Rush Univeristy Medical Center Chicago, Illinois, United States, 60612 收起 <<
NCT03608085 Heart Failure Not Applicable Recruiting May 31, 2019 United States, Rhode Island ... 展开 >> Ocean State Research Institute Recruiting Providence, Rhode Island, United States, 02908 Contact: Mary Ford    401-273-7100 ext 3674    Mary.Ford@va.gov    Principal Investigator: Tracey H Taveira, Pharm.D.          Sub-Investigator: Philip Haines, MD          Sub-Investigator: Wen-Chih Wu, MD          Providence VAMC Recruiting Providence, Rhode Island, United States, 02908 Contact: Melanie R Parent, Ba    401-273-7100 ext 6293    Melanie.Parent@va.gov    Principal Investigator: Tracey H Taveira, Pharm.D. 收起 <<
NCT03619317 - Recruiting August 2020 Denmark ... 展开 >> University Hospital of Aarhus, Department of Cardiology Recruiting Aarhus N, Denmark, 8200 Contact: Mette Søndergaard    30130565    metast@rm.dk    Contact: Steen Poulsen       steen.hvitfeldt@rm.dk 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.09mL

1.02mL

0.51mL

25.43mL

5.09mL

2.54mL

50.86mL

10.17mL

5.09mL
参考文献

[1]Mazari L, Ouarzane M, et al. Subversion of B lymphocyte tolerance by hydralazine, a potential mechanism for drug-induced lupus. Proc Natl Acad Sci U S A. 2007 Apr 10;104(15):6317-22. Epub 2007 Apr 2.

[2]Burcham PC, Pyke SM. Hydralazine inhibits rapid acrolein-induced protein oligomerization: role of aldehyde scavenging and adduct trapping in cross-link blocking and cytoprotection. Mol Pharmacol. 2006 Mar;69(3):1056-65.

[3]Bourreli B, Pinaud M, Passuti N, Gunst JP, Drouet JC, Remi JP. Additive effects of dihydralazine during enflurane or isoflurane hypotensive anaesthesia for spinal fusion. Can J Anaesth. 1988;35(3 ( Pt 1)):242-248

[4]Kandler MR, Mah GT, Tejani AM, Stabler SN. Hydralazine for essential hypertension. Cochrane Database Syst Rev. 2010;(8):CD004934. Published 2010 Aug 4

[5]Genedy S, Khames A, Hussein A, Sarhan H. Hydralazine HCl rapidly disintegrating sublingual tablets: simple dosage form of higher bioavailability and enhanced clinical efficacy for potential rapid control on hypertensive preeclampsia. Drug Des Devel Ther. 2018;12:3753-3766. Published 2018 Nov 5

[6]Ferdinand KC. Isosorbide dinitrate and hydralazine hydrochloride: a review of efficacy and safety. Expert Rev Cardiovasc Ther. 2005;3(6):993-1001