67227-56-9
Chemical Structure
Fenoldopam
Synonym(s): SKF 82526
- CAS No.: 67227-56-9
- Formula:C16H16ClNO3
- Molecular Weight:305.76
IUPAC Name: 6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol
InChIKey: TVURRHSHRRELCG-UHFFFAOYSA-N
SMILES: OC1=C(O)C=C2C(C3=CC=C(O)C=C3)CNCCC2=C1Cl
Biological Activity: 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[1][2][3][4][5][6][7][8].
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Fenoldopam | 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. | |||||||||||||||||||||
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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]
