Fenoldopam (mesylate)
(Synonyms: 非诺多泮甲磺酸盐; Fenoldopam methanesulfonate; SKF-82526 mesylate) 目录号 : GC43660
An agonist of dopamine D1A and D1B receptors
Cas No.:67227-57-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with natriuretic/diuretic properties. Fenoldopam stimulated cAMP accumulation in LLC-PK1 cells in a dose-dependent manner, an effect which could be blocked by the DA1-selective antagonist Sch 23390. Although fenoldopam was more potent than DA (EC50 55.5 +/- 7.75 nM vs. 1.65 +/- 0.64 microM) in stimulating cAMP accumulation in LLC-PK1 cells, the maximum stimulation obtained by fenoldopam was only 37% of the maximum stimulation obtained by DA(Emax 13.0 +/- 2.95 pmol/mg of protein vs. 35.6 +/- 10.19 pmol/mg of protein) [1]. Fenoldopam is a selective dopamine1 (DA1) receptor agonist. Most of the DA1 receptor agonist activity of fenoldopam resides in the R-enantiomer, which also shows weaker alpha 2-adrenoceptor antagonist activity Fenoldopam produces vasodilation in vascular beds that are rich in vascular DA1 receptors [2].
References:
[1]. Grenader, A. and D.P. Healy, Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells. J Pharmacol Exp Ther, 1991. 258(1): p. 193-8.
[2]. Nichols, A.J., R.R. Ruffolo, Jr., and D.P. Brooks, The pharmacology of fenoldopam. Am J Hypertens, 1990. 3(6 Pt 2): p. 116S-119S.
| Cas No. | 67227-57-0 | SDF | |
| 别名 | 非诺多泮甲磺酸盐; Fenoldopam methanesulfonate; SKF-82526 mesylate | ||
| Canonical SMILES | OC(C=C1)=CC=C1C2CNCCC3=C2C=C(O)C(O)=C3Cl.CS(=O)(O)=O | ||
| 分子式 | C16H16ClNO3•CH3SO3H | 分子量 | 401.9 |
| 溶解度 | DMF: 2 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 1 mg/ml,Ethanol: 0.25mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4882 mL | 12.4409 mL | 24.8818 mL |
| 5 mM | 0.4976 mL | 2.4882 mL | 4.9764 mL |
| 10 mM | 0.2488 mL | 1.2441 mL | 2.4882 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Fenoldopam mesylate: A Narrative Review of Its Use in Acute Kidney Injury
Curr Pharm Biotechnol 2019;20(5):366-375.PMID:31038062DOI:10.2174/1389201020666190417124711.
Background: Fenoldopam mesylate is a selective agonist of DA-1 receptors. It is currently used for the in-hospital treatment of severe hypertension. DA-1 receptors have high density in renal parenchyma and for this reason, a possible reno-protective role of Fenoldopam mesylate was investigated. Methods: We examined all studies regarding the role of Fenoldopam mesylate in Acute Kidney Injury (AKI); particularly, those involving post-surgical patients, intensive care unit patients and contrastinduced nephropathy. Results: Fenoldopam mesylate was found to be effective in reducing the onset of postoperative AKI, when used before the development of the kidney damage. Positive results were also obtained in the management of intensive care unit patients with AKI, although the clinical studies investigated were few and conducted on small samples. Conclusion: Conflicting results were achieved in contrast-induced nephropathy.
Fenoldopam mesylate for treating psoriasis: A new indication for an old drug
Int J Pharm 2020 Jan 5;573:118726.PMID:31715365DOI:10.1016/j.ijpharm.2019.118726.
Fenoldopam, a highly selective dopamine receptor agonist, is available in clinics as Corlopam™ i.v. for the management of severe hypertension. Recent reports demonstrate its anti-proliferative activity in vitro in a dose dependent manner. However, stability issues of the drug due to its susceptibility to oxidation, pH sensitivity, poor transdermal flux, and the barrier properties of skin present challenges to develop a topical formulation of Fenoldopam. The aim of the present study is to suggest a stable topical formulation of Fenoldopam for the treatment of psoriasis. Water washable ointment and glycerin-based carbopol anhydrous gel of Fenoldopam intended for topical delivery were prepared and evaluated in vitro and in vivo. Results from pH dependent stability studies suggest the necessity to maintain acidic pH in final formulations. The presence of an acidic adjuster in ointment and unneutralised carbopol dispersion of anhydrous gel maintain the desired acidic environment in the formulations. Stability studies of prepared formulations performed for 90 days indicate that the drug remains stable in formulations. In vivo studies demonstrate the applicability of the formulations for better skin penetration, skin compliance, and photosafety. Efficacy studies using an imiquimod induced psoriasis model confirm the promising application of developed Fenoldopam topical formulations for psoriasis.
Contrast-induced nephropathy
J Vasc Surg 2011 Aug;54(2):575-9.PMID:21741789DOI:10.1016/j.jvs.2011.04.047.
Contrast-induced nephropathy (CIN) has been extensively studied since the 1950s due, in part, to its devastating adverse events. The intellectual push for additional investigation into pathogenesis and prevention has heightened in recent years due to increased utilization of contrast enhanced imaging studies. Lack of a universal CIN definition and varied glomerular filtration rate markers have resulted in a varied reported incidence. Risk assessment and risk reduction strategies have evolved over the past several years. Current evidence supports volume supplementation before the administration of intravascular contrast to reduce the hazard of CIN. Other strategies to reduce the risk of CIN, including low osmolar contrast media, N-acetylcysteine, and intrarenal Fenoldopam therapy, have variable levels of evidence, and further randomized trials are necessary.
Fenoldopam mesylate Enhances the Survival of Mesenchymal Stem Cells Under Oxidative Stress and Increases the Therapeutic Function in Acute Kidney Injury
Cell Transplant 2023 Jan-Dec;32:9636897221147920.PMID:36594258DOI:10.1177/09636897221147920.
Mesenchymal stem cells (MSCs) have gained interest as an alternative therapeutic option for renal diseases, including acute kidney injury (AKI). However, their use is often limited owing to low survival rates in vivo. Fenoldopam mesylate (FD) is a selective dopamine D1 receptor agonist with antioxidative and anti-apoptotic roles. Herein, we investigated whether FD can enhance the survival of MSCs undergoing oxidative stress in vitro. In addition, the therapeutic effect of MSCs and FD-treated MSCs (FD-MSCs) was compared in a mouse model of AKI induced by cisplatin. The survival of MSCs under oxidative stress was augmented by FD treatment. FD induced the phosphorylation of cAMP response element-binding protein and AKT, contributing to enhanced growth compared with untreated MSCs. The expression of nuclear factor erythroid-2-related factor 2 (NRF2) and heme oxygenase-1 was increased by FD treatment, and nuclear translocation of NRF2 was found exclusively in FD-MSCs. FD downregulated BAX expression, increased the mitochondrial membrane potential, reduced reactive oxygen species generation, and decreased the apoptotic death of MSCs induced by oxidative stress. Moreover, renal function and tubular injury were improved in FD-MSCs compared with non-treated MSCs. Furthermore, tubular injury, apoptosis, and macrophage infiltration, as well as the serum level of tumor necrosis factor-α were reduced, while tubular cell proliferation was markedly increased in FD-MSCs compared with MSCs. Our study demonstrated that FD increases the survivability of MSCs in an oxidative environment, and its use may be effective in preparing robust therapeutic MSCs.
Fenoldopam mesylate blocks reductions in renal plasma flow after radiocontrast dye infusion: a pilot trial in the prevention of contrast nephropathy
Am Heart J 2002 May;143(5):894-903.PMID:12040355DOI:10.1067/mhj.2002.122118.
Background: Radiocontrast nephropathy (RCN) is a common source of acute renal failure in hospitalized patients and is associated with increased morbidity and mortality rates. Fenoldopam mesylate is a dopamine A1 receptor agonist that augments renal plasma flow (RPF) in patients with normotensive and hypertensive conditions. To determine whether Fenoldopam mesylate attenuates reductions in RPF after contrast infusion, we conducted a double-blind, randomized, placebo-controlled pilot trial of Fenoldopam mesylate in patients who underwent contrast angiography. Methods: Fifty-one patients with chronic renal insufficiency (creatinine level, 2.0-5.0 mg/dL) who were undergoing contrast angiography were screened, and 45 patients were randomized to receive normal saline solution (1/2 NS) or 1/2 NS plus Fenoldopam mesylate at 0.1 microg/kg/min at lease 1 hour before infusion with contrast dye. Serum creatinine level was measured at baseline and at 24, 48, and 72 hours after angiography. The primary endpoint was change in RPF 1 hour after contrast infusion. The secondary endpoint was incidence of RCN, defined as a 0.5 mg/dL or a 25% rise in serum creatinine level at 48 hours. Results: RPF at 1 hour after angiography was 15.8% above baseline in the Fenoldopam mesylate group compared with 33.2% below baseline in the 1/2 NS group (P <.05). The incidence rate of RCN at 48 hours was 41.0% in the 1/2 NS group versus 21% in the Fenoldopam mesylate group (P =.148). Among patients with diabetes, the incidence rate of RCN tended to be higher in the 1/2 NS group compared with the Fenoldopam mesylate group (64% vs 33%; P =.14). The peak serum creatinine level at 72 hours after contrast infusion was significantly higher at in the 1/2 NS group (creatinine level, 3.6 +/- 1.0 mg/dL) compared with the Fenoldopam mesylate group (creatinine level, 2.8 +/- 0.35 mg/dL; P <.05). RPF was significantly (P <.0001) reduced in patients with RCN compared with patients in whom RCN did not develop. Conclusion: The results of this pilot trial suggest that Fenoldopam mesylate is a promising prophylactic agent for RCN and that larger multicenter trials should be conducted to prove its efficacy.