SKF38393 HCl (Synonyms: (±)-SKF-38393 hydrochloride; SKF-38393A) |
رقم الكتالوجGC17729
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SKF38393 HCl هو ناهض انتقائي لمستقبل الدوبامين D1 (D1DR) مع IC50 من 110 نانومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 62717-42-4
Sample solution is provided at 25 µL, 10mM.
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.
| Cas No. | 62717-42-4 | SDF | |
| المرادفات | (±)-SKF-38393 hydrochloride; SKF-38393A | ||
| Chemical Name | 1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrochloride | ||
| Canonical SMILES | OC1=C(O)C=C2C(CCNCC2C3=CC=CC=C3)=C1.Cl | ||
| Formula | C16H18ClNO2 | M.Wt | 291.77 |
| الذوبان | ≥ 29.2 mg/mL in DMSO, ≥ 3 mg/mL in EtOH with ultrasonic and warming, ≥ 14.75 mg/mL in Water with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4274 mL | 17.1368 mL | 34.2736 mL |
| 5 mM | 685.5 μL | 3.4274 mL | 6.8547 mL |
| 10 mM | 342.7 μL | 1.7137 mL | 3.4274 mL |
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)