SKF38393 HCl
(Synonyms: (±)-SKF-38393 hydrochloride; SKF-38393A) 目录号 : GC17729
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
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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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.
| Cas No. | 62717-42-4 | SDF | |
| 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 SMILES | OC1=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4274 mL | 17.1368 mL | 34.2736 mL |
| 5 mM | 0.6855 mL | 3.4274 mL | 6.8547 mL |
| 10 mM | 0.3427 mL | 1.7137 mL | 3.4274 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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