Fenoldopam mesylate

Research use only, not for human use.

Fenoldopam is a selective dopamine-1 receptor (DA1) agonist with natriuretic/diuretic properties. It lowers blood pressure through arteriolar vasodilation.

Fenoldopam mesylate is a synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. Fenoldopam is used as an antihypertensive agent. It was approved by the Food and Drug Administration (FDA) in September 1997. Since fenoldopam is the only intravenous agent that improves renal perfusion, in theory it could be beneficial in hypertensive patients with concomitant renal insufficiency.(In Vitro):Fenoldopam is a partial agonist with low efficacy at DA1 receptors linked to cAMP generation in the LLC-PK1 cells.Fenoldopam (0-300 μM; 48 or 72 h) displays significant antiproliferative activity against RCC cell lines.Fenoldopam (5 μM and 10 μM; 72 h) induces cell apoptosis in a dose-dependent manner.(In Vivo):Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can induce arteritis in rats detected by magnetic resonance imaging (MRI).

Fenoldopam is a partial agonist with low efficacy at DA1 receptors linked to cAMP generation in the LLC-PK1 cells.Fenoldopam (0-300 μM; 48 or 72 h) displays significant antiproliferative activity against RCC cell lines. Fenoldopam (5 μM and 10 μM; 72 h) induces cell apoptosis in a dose-dependent manner. Cell Proliferation Assay Cell Line:786-O, ACHN, and HK-2 cells Concentration:0-300 μM Incubation Time:48 or 72 hours Result:Inhibited the growth of ACHN cells (IC50=16.55 μM, 48 h; IC50=10.34 μM, 72 h), 786-O cells (IC50=57.89 μM, 48 h; IC50=47.52 μM, 72 h), and HK2 cells (IC50>300 μM, 48h and 72 h).Apoptosis AnalysisCell Line:ACHN cells Concentration:5 μM and 10 μM Incubation Time:72 hours Result:Increased apoptotic cells from at 2.2% (control) to 47.7% (5 μM, fenoldopam) and 60.8% (10 μM, fenoldopam), respectively.

Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can induce arteritis in rats detected by magnetic resonance imaging (MRI). Animal Model:Female Sprague-Dawley rats Dosage:100 mg/kg Administration:Subcutaneous injection; 100 mg/kg; once daily; 2 days Result:Showed low-intensity areas and a high signal intensity region around the artery, and these findings were considered to be erythrocytes infiltrating the arterial wall and perivascular edema, respectively.Observed perivascular edema histopathologically.

Fenoldopam, Corlopam, SK and F-82526J

Others

Other Targets

dopamine-1 receptor

Cardiovascular Disease

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67227-57-0

401.86

C16H16ClNO3·CH4O3S

>98% (HPLC)

DMSO : ≥ 36 mg/mL 89.58 mM; H2O : 10 mg/mL24.88 mM

CS(O)(=O)=O.OC1=CC=C(C=C1)C1CNCCC2=C(Cl)C(O)=C(O)C=C12

9-chloro-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol

(-20℃)

With Ice Pack

≥ 2 years