80751-85-5
Chemical Structure
SKF 83959
- CAS No.: 80751-85-5
- Formula:C18H20ClNO2
- Molecular Weight:317.81
IUPAC Name: 6-chloro-3-methyl-1-(m-tolyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol
InChIKey: JXMYTVOBSFOHAF-UHFFFAOYSA-N
SMILES: OC1=C(O)C=C2C(C3=CC=CC(C)=C3)CN(C)CCC2=C1Cl
Biological Activity: SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression[1][2][3][4].
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SKF 83959 | 98.30% | SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression. | ||||||||||||||||||||
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SKF83822 hydrobromide | SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors. | |||||||||||||||||||||
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SKF 83959 hydrobromide | 99.86% | SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression. | ||||||||||||||||||||
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SKF-82958 | SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM). | |||||||||||||||||||||
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SKF-82958 hydrobromide (Standard) | ≥98% | SKF-82958 (hydrobromide) (Standard) is the analytical standard of SKF-82958 (hydrobromide). This product is intended for research and analytical applications. SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM). | ||||||||||||||||||||
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Fenoldopam hydrochloride | Fenoldopam (SKF 82526) hydrochloride is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam hydrochloride shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis. | |||||||||||||||||||||
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SKF 83822 | 98.01% | SKF 83822 is an atypical agonist of dopamine D1 receptor. SKF 83822 activates adenylyl cyclase (AC), but not phospholipase C (PLC). SKF 83822 is also proved to stimulate AC via cAMP production. SKF 83822 can be used for research of schizophrenia. | ||||||||||||||||||||
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SKF 81297 hydrobromide | 99.88% | SKF 81297 hydrobromide is a potent and selective dopamine D1 receptor agonist. | ||||||||||||||||||||
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SKF 81297 | 99.68% | SKF 81297 is a potent and selective dopamine D1 receptor agonist. | ||||||||||||||||||||
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(R)-SKF-81297 hydrobromide | (R)-SKF-81297 hydrobromide is the R-enantiomer of SKF-81297 (HY-12236A). SKF-81297 is a selective agonist for dopamine D1 receptor. | |||||||||||||||||||||
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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]. Sheng G, et al. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia. Biol Pharm Bull. 2018;41(3):427-434. [Content Brief]
- [2]. Jin LQ, et al. SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain. J Neurochem. 2003;85(2):378-386. [Content Brief]
- [3]. Neumeyer JL, et al. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur J Pharmacol. 2003;474(2-3):137-140. [Content Brief]
- [4]. Guo L, et al. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol Pharmacol. 2013;83(3):577-586. [Content Brief]