SKF38393 HCldopamine D1 receptor agonist CAS# 62717-42-4 |
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Quality Control & MSDS
3D structure
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| Cas No. | 62717-42-4 | SDF | Download SDF |
| PubChem ID | 147514 | Appearance | Powder |
| Formula | C16H18ClNO2 | M.Wt | 291.77 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 34 mg/mL (116.53 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;hydrochloride | ||
| SMILES | C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3.Cl | ||
| Standard InChIKey | YEWHJCLOUYPAOH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H17NO2.ClH/c18-15-8-12-6-7-17-10-14(13(12)9-16(15)19)11-4-2-1-3-5-11;/h1-5,8-9,14,17-19H,6-7,10H2;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
SKF38393 HCl Dilution Calculator
SKF38393 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.4274 mL | 17.1368 mL | 34.2736 mL | 68.5471 mL | 85.6839 mL |
| 5 mM | 0.6855 mL | 3.4274 mL | 6.8547 mL | 13.7094 mL | 17.1368 mL |
| 10 mM | 0.3427 mL | 1.7137 mL | 3.4274 mL | 6.8547 mL | 8.5684 mL |
| 50 mM | 0.0685 mL | 0.3427 mL | 0.6855 mL | 1.3709 mL | 1.7137 mL |
| 100 mM | 0.0343 mL | 0.1714 mL | 0.3427 mL | 0.6855 mL | 0.8568 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SKF38393 HCl (SKF38393) is a selective dopamine D1 receptor agonist [1], with an IC50 value of 110 nM [2].
There are two functional types of dopamine receptors, D1 and D2 receptors [3]. The stimulation of the D1 receptor (D1R) in prefrontal cortex (PFC) results in an ‘inverted-U’ dose-response. Either too little or too much D1R stimulation can impair spatial working memory [4].
6-OHDA reduced the specific expression of mRNAs to encode substance P and D1 dopamine receptor in striatonigral neurons. Subsequently daily injections of SKF-38393 reversed this reduction effect. The treatment with SKF-38393 also increased dynorphin mRNA [5]. D1Rs activate cyclic AMP-dependent protein kinases, stimulate adenylyl cyclase, regulate neuron growth and differentiation, modify dopamine D2 receptor-mediated events and influence behavior [3]. In a 96-well plate assay, the plating of MCF-7 cells was involved in the breast cancer in vitro screening procedure. After 1 day, treatment with SKF 38393 was applied to cells for 2 days. Data showed that SKF 38393 significantly decrease the proliferation of MCF-7 cells. The IC50 value was 0.1 +/- 0.03 µM [6].
In locally anesthetized, artificially respired, gallamine-treated rats, i.v. administration of SKF 38393 significantly altered dopamine cell activity. In these rats, firing rate increases and decreases were also observed [7].
References:
[1]. Rimondini R, Ferré S, Giménez-Llort L, et al. Differential effects of selective adenosine A1 and A2A receptor agonists on dopamine receptor agonist-induced behavioral responses in rats. European journal of pharmacology, 1998, 347(2): 153-158.
[2]. Altar CA, Marien MR. Picomolar affinity of 125I-SCH 23982 for D1 receptors in brain demonstrated with digital subtraction autoradiography. The Journal of neuroscience, 1987, 7(1): 213-222.
[3]. Sunahara RK, Niznik HB, Weiner DM, et al. Human dopamine D1 receptor encoded by an intronless gene on chromosome 5. 1990, 347:80-83.
[4]. Vijayraghavan S, Wang M, Birnbaum SG, et al. Inverted-U dopamine D1 receptor actions on prefrontal neurons engaged in working memory. Nature neuroscience, 2007, 10(3): 376-384.
[5]. Gerfen CR, Engber TM, Mahan LC, et al. D1 and D2 dopamine receptor-regulated gene expression of striatonigral and striatopallidal neurons. Science, 1990, 250(4986): 1429-1432.
[6]. Johnson DE, Ochieng J, Evans SL. The growth inhibitory properties of a dopamine agonist (SKF 38393) on MCF-7 cells. Anti-cancer drugs, 1995, 6(3): 471-474.
[7]. Carlson JH, Bergstrom DA, Weick BG, et al. Neurophysiological investigation of effects of the D-1 agonist SKF 38393 on tonic activity of substantia nigra dopamine neurons. Synapse, 1987, 1(5): 411-416.
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