Fenoldopam
Based on 4 publication(s) in Google Scholar
Fenoldopam (SKF-82526) is a selective dopamine D1 receptor agonist. Fenoldopam binds to rat D1B dopamine receptors (Kd = 11 nM) and human D1A receptors (Kd = 17 nM) in COS-7 cell membranes expressing the cloned receptors. Fenoldopam modulates dopamine receptor expression, induces vasorelaxation in vascular tissues, reverses glomerular hyperfiltration in rat models, increases intracellular cAMP levels, promotes DARPP-32 phosphorylation in small cell lung cancer (SCLC) cells, inhibits cytokine secretion, and downregulates T cell activation markers in activated human T cells. Fenoldopam can be used for research on hypertension, acute kidney injury, psoriasis, and small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 67227-56-9
- Formula: C16H16ClNO3
- Molecular Weight:305.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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HY-B0410
Pramipexole
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HY-B0735A
Fenoldopam mesylate
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HY-14763
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Bromocriptine mesylate
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Pramipexole dihydrochloride
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Cariprazine hydrochloride
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HY-A0007
Rotigotine Hydrochloride
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HY-19545A
SCH-23390 hydrochloride
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HY-B0735AR
Fenoldopam mesylate (Standard)
Publications Citing Use of MedChemExpress (MCE) Fenoldopam
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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Human D1 Receptor 17 nM (Kd) |
Rat D1 Receptor 11 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LLC-PK1 | EC50 |
55.5 nM
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Stimulates cAMP accumulation.
Stimulates cAMP accumulation.
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2973247 |
Fenoldopam (SKF-82526) (40 min) competes for specific 125I-Sch 23982 binding sites in rat renal cortical membranes with a Ki of 1,975 nM (Tris-HCl buffer) and 1,895 nM (Dulbecco's buffer)[1].
Fenoldopam (1 nM-6 μM; 72 h) does not inhibit the proliferation of CD3/CD28-stimulated Jurkat leukemic T cells, in contrast to its inhibitory effect on normal activated T cells[2].
Fenoldopam (1 μM; 5 h) co-treated Theophylline (HY-B0809) increases intracellular cAMP levels in CD3/CD28-stimulated Jurkat cells[2].
Fenoldopam (1 μM; 10-30 min) increases DARPP-32 phosphorylation in small cell lung cancer (SCLC) H-69 cells and primary SCLC cultures[3].
Fenoldopam (1 μM; 30 180 min) induces cAMP accumulation in SCLC cells and increases BrdU incorporation in SCLC H-69 cells as well as primary SCLC cultures (SCLC H-3)[3].
Fenoldopam (0.1 μM; 48 h) reduces the secretion of TNF-α, IFN-γ, IL-1β, IL-2, IL-4, IL-6, IL-8 and IL-10 by IL-2 activated PBMCs, and downregulates the expression of T cell activation markers CD69, CD28 and intracellular IL-2 in CD3+ T cells from psoriasis patients[4].
Fenoldopam (0.1 μM; 1 h) reduces the chemotactic migration of CD3/CD28-activated normal human T cells towards SDF-1/CXCL12 by 27-55%[4].
Fenoldopam (0.1 μM; 15 sec) induces depolarization of resting and activated normal human T cells[4].
Fenoldopam (10 pM-1 μM; 24 h) increases D1 and D3 receptor protein expression in a concentration- and time-dependent manner in rat aortic smooth muscle A10 cells[6].
Fenoldopam (0.1 μM; 24 h) increases D1/D3 receptor coimmunoprecipitation in A10 cells[6].
Fenoldopam (100 pM-1 mM) induces vasorelaxation in rat mesenteric arterial rings preconstricted with KCl (Emax = 83%, pED50 = 5.0)[6].
Fenoldopam binds to rat D1B dopamine receptors with a Kd of 11 nM and human D1A receptors with a Kd of 17 nM in COS-7 cell membranes expressing the cloned receptors[7].
Fenoldopam (1 nM-100 μM; cumulative) has minimal effect on mouse ductus arteriosus tone, and does not impair O2-or indomethacin-induced ductus constriction[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat leukemic T cells, normal activated T cells
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Concentration:1, 5, 10, 50, 100, 200, 400, 600, 800 nM; 1, 2, 4, 6 μM
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Incubation Time:72 h
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Result:Did not inhibit proliferation of CD3/CD28-stimulated Jurkat cells at any concentration tested.
Inhibited proliferation of normal activated T cells with maximum inhibition at 1 μM.
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Cell Line:SCLC H-69 cells, SCLC primary cultures
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Concentration:1 μM
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Incubation Time:10, 30 min
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Result:Increased DARPP-32 phosphorylation.
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Cell Line:SCLC H-69 cells, SCLC primary cultures (SCLC-H3)
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Concentration:1 μM
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Incubation Time:30, 90, 180 min
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Result:Induced BrdU incorporation in both cell lines.
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Cell Line:CD3/CD28-activated normal human T cells
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Concentration:100 nM
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Incubation Time:1 h pre-incubation + 4 h migration assay
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Result:Reduced chemotactic migration towards SDF-1/CXCL12 by 27-55%.
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Cell Line:A10 cells (rat aortic smooth muscle cells)
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Concentration:10 pM-1 μM
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Incubation Time:24 h (concentration-response); 2, 4, 8, 16, 24, 30 h (time-course)
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Result:Increased D1 and D3 receptor protein expression in a concentration- and time-dependent manner.
Fenoldopam (1, 3, 10 μg/kg; i.v.; 40 min per dose) increases effective renal plasma flow (ERPF) in a dose-dependent manner in conscious rats, with no significant change in GFR, resulting in a decreased filtration fraction[5].
Fenoldopam (1 mg/kg; i.p.; once hourly for 4 doses) does not impair postnatal ductus arteriosus closure in newborn CD-1 mice[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Glycine-induced hyperfiltration study in conscious male SD rats (320-360 g)[5]
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Dosage:1 μg/kg
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Administration:i.v.; during glycine infusion
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Result:Reversed glycine-induced glomerular hyperfiltration and reduced GFR from 1.30 to 1.17 mL/100 g/min.
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Animal Model:Dose-response study in conscious male SD rats (320-360 g)[5]
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Dosage:1, 3, 10 μg/kg
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Administration:i.v.; 40 min per dose
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Result:Increased effective renal plasma flow (ERPF) in a dose-dependent manner in conscious rats, with no significant change in GFR, resulting in a decreased filtration fraction.
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Animal Model:Postnatal ductus arteriosus closure study in newborn CD-1 mice[8]
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Dosage:1 mg/kg
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Administration:i.p.; once hourly for 4 doses
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Result:Did not impair postnatal ductus arteriosus closure.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 67227-56-9
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Molecular Weight 305.76
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Formula C16H16ClNO3
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SMILES
OC1=C(O)C=C2C(C3=CC=C(O)C=C3)CNCCC2=C1Cl
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Synonyms
SKF 82526
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell
2021 Feb 18;184(4):943-956.e18. PMID: 33571432 -
SLAS Discov
2020 Sep;25(8):895-905. PMID: 32567455 -
Biochem Biophys Res Commun
2022 Jan 15:588:83-89. PMID: 34953210 -
Biomed Pharmacother
Dopamine receptor agonists ameliorate bleomycin-induced pulmonary fibrosis by repressing fibroblast differentiation and proliferation. [Abstract]2021 Jul:139:111500. PMID: 33901873
Purity & Documentation
References
[1]. Felder RA, et al. Dopamine1 receptors in rat kidneys identified with 125I-Sch 23982. Am J Physiol. 1988 Nov;255(5 Pt 2):F970-6. [Content Brief]
[2]. Basu B, et al. D1 and D2 dopamine receptor-mediated inhibition of activated normal T cell proliferation is lost in jurkat T leukemic cells. J Biol Chem. 2010 Aug 27;285(35):27026-27032. [Content Brief]
[3]. Cherubini E, et al. Genetic and Functional Analysis of Polymorphisms in the Human Dopamine Receptor and Transporter Genes in Small Cell Lung Cancer. J Cell Physiol. 2016 Feb;231(2):345-56. [Content Brief]
[4]. Keren A, et al. Instantaneous depolarization of T cells via dopamine receptors, and inhibition of activated T cells of Psoriasis patients and inflamed human skin, by D1-like receptor agonist: Fenoldopam. Immunology. 2019 Nov;158(3):171-193. [Content Brief]
[5]. Gillies MA, et al. Fenoldopam to prevent acute kidney injury after major surgery-a systematic review and meta-analysis. Crit Care. 2015 Dec 25;19:449. [Content Brief]
[6]. Zeng C, et al. Dopamine D1 receptor augmentation of D3 receptor action in rat aortic or mesenteric vascular smooth muscles. Hypertension. 2004 Mar;43(3):673-9. [Content Brief]
[7]. Tiberi M, et al. Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor. Proc Natl Acad Sci U S A. 1991 Sep 1;88(17):7491-5. [Content Brief]
[8]. Crockett SL, et al. Role of dopamine and selective dopamine receptor agonists on mouse ductus arteriosus tone and responsiveness. Pediatr Res. 2020 May;87(6):991-997. [Content Brief]
Calculators
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