Clevidipine

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Chemical Structure| 167221-71-8 同义名 : 氯维地平 ;rac-Clevidipine;Clevidipine Butyrate;Clevelox;167221-71-8;Cleviprex
CAS号 : 167221-71-8
货号 : A387256
分子式 : C21H23Cl2NO6
纯度 : 97%
分子量 : 456.316
MDL号 : MFCD00940070
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(109.57 mM)，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
靶点

  • Calcium Channel
描述 Clevidipine is a short-acting dihydropyridine calcium channel antagonist. Clevidipine is an ultrashort-acting drug for rapid reduction of blood pressure by selectively acting on the L-type Ca2+ channels on arteriolar smooth muscle. The drug's ultrashort action in reducing the blood pressure is due to its rapid hydrolysis by blood and extravascular tissue esterases, which does not depend on hepato-renal metabolism and excretion[3]. When myocytes were voltage-clamped with holding potential (VH) at -80 mV, 10 nM clevidipine decreased ICa at 0 mV by approximately 30%, but >50% when VH was -40 mV[4]. Clevidipine is an endothelium-independent arterial vasodilator that offers a potential therapeutic option in the treatment of perioperative arterial graft vasospasm and/or hypertension[2]. Clevidipine provided rapid BP control in patients with acute neurological injuries (including intracerebral haemorrhage, subarachnoid haemorrhage and acute ischaemic stroke), and was not associated with 'overshoot' in the vast majority of patients. Intravenous clevidipine was generally well tolerated and was usually associated with no reflex tachycardia or only very modest increases in heart rate[5]. Clevidipine administration during initial medical management of aortic dissection showed similar efficacy compared to SNP (sodium nitroprusside) when used as adjunct therapy to esmolol[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
NCT01369147 Critical Illness Phase 2 Suspended(The study has been h... 展开 >>alted pending additional funding.) 收起 << October 2019 United States, Georgia ... 展开 >> Emory University Hospital Atlanta, Georgia, United States, 30322 收起 <<
NCT03719001 Vascular Diseases Early Phase 1 Recruiting October 1, 2020 United States, California ... 展开 >> University of California San Francisco Recruiting San Francisco, California, United States, 94122 Contact: Pekka Talke, MD    415-476-8963    pekka.talke@ucsf.edu    Contact: Pekka Talke, MD    415-476-8963    talkep@anesthesia.ucsf.edu 收起 <<
NCT01033370 Aortic Aneurysm ... 展开 >> Aortic Disease 收起 << Phase 4 Terminated(Project lacked fund... 展开 >>ing.) 收起 << - United States, Texas ... 展开 >> The Methodist Hospital Houston, Texas, United States, 77030 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.96mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL
参考文献

[1]Ericsson H, Tholander B, et al. In vitro hydrolysis rate and protein binding of clevidipine, a new ultrashort-acting calcium antagonist metabolised by esterases, in different animal species and man. Eur J Pharm Sci. 1999 Apr;8(1):29-37.

[2]Huraux C, Makita T, Szlam F, Nordlander M, Levy JH. The vasodilator effects of clevidipine on human internal mammary artery. Anesth Analg. 1997;85(5):1000‐1004

[3]Espinosa A, Ripollés-Melchor J, Casans-Francés R, et al. Perioperative Use of Clevidipine: A Systematic Review and Meta-Analysis. PLoS One. 2016; 11(3):e0150625. Published 2016 Mar 28

[4]Yi X, Vivien B, Lynch C 3rd. Clevidipine blockade of L-type Ca2+ currents: steady-state and kinetic electrophysiological studies in guinea pig ventricular myocytes. J Cardiovasc Pharmacol. 2000; 36(5):592‐600

[5]Keating GM. Clevidipine: a review of its use for managing blood pressure in perioperative and intensive care settings. Drugs. 2014;74(16):1947‐1960

[6]Ulici A, Jancik J, Lam TS, Reidt S, Calcaterra D, Cole JB. Clevidipine versus sodium nitroprusside in acute aortic dissection: A retrospective chart review. Am J Emerg Med. 2017; 35(10):1514‐1518