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SKF38393 HCl
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SKF38393 HCl图片
CAS NO:62717-42-4
包装与价格：
包装价格(元)
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SKF38393 HCl 是一种多巴胺 D1 受体 (D1DR) 的选择性激动剂，IC50 为 110 nM。
Cas No.62717-42-4
别名(±)-SKF-38393 hydrochloride; SKF-38393A
化学名1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrochloride
Canonical SMILESOC1=C(O)C=C2C(CCNCC2C3=CC=CC=C3)=C1.Cl
分子式C16H18ClNO2
分子量291.77
溶解度≥ 29.2 mg/mL in DMSO, ≥ 3 mg/mL in EtOH with ultrasonic and warming, ≥ 14.75 mg/mL in Water with ultrasonic
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

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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