MLS-1547
目录号 : GC45676
An agonist of dopamine D2 receptors
Cas No.:315698-36-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MLS-1547 is a G protein-biased agonist of dopamine D2 receptors (EC50 = 0.37 μM in a calcium mobilization assay).1 It inhibits forskolin-induced cAMP accumulation in CHO cells expressing human D2 receptors (EC50 = 0.26 μM) but is inactive in β-arrestin recruitment assays. MLS-1547 antagonizes dopamine-induced β-arrestin recruitment in cell-based assays with IC50 values ranging from 3.8 to 9.9 μM.1 It is also an inhibitor of type II secretion in Gram-negative bacteria.2 MLS-1547 inhibits secretion of phospholipase C (PlcH/N) and the virulence factor elastase (LasB) from P. aeruginosa (IC50s = 15 and 13 μM, respectively) and inhibits B. pseudomallei protease secretion by 90.8% when used at a concentration of 25 μM.
|1. Free, R.B., Chun, L.S., Moritz, A.E., et al. Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol. Pharmacol. 86(1), 96-105 (2014).|2. Moir, D.T., Di, M., Wong, E., et al. Development and application of a cellular, gain-of-signal, bioluminescent reporter screen for inhibitors of type II secretion in Pseudomonas aeruginosa and Burkholderia pseudomallei. J. Biomol. Screen. 16(7), 694-705 (2011).
| Cas No. | 315698-36-3 | SDF | |
| Canonical SMILES | OC1=C(C=C(Cl)C2=C1N=CC=C2)CN(CC3)CCN3C4=CC=CC=N4 | ||
| 分子式 | C19H19ClN4O | 分子量 | 354.8 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml | 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 | 2.8185 mL | 14.0924 mL | 28.1849 mL |
| 5 mM | 0.5637 mL | 2.8185 mL | 5.637 mL |
| 10 mM | 0.2818 mL | 1.4092 mL | 2.8185 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Prefrontal Dopaminergic Regulation of Cue-Guided Risky Decision-Making Performance in Rats
Front Behav Neurosci 2022 Jul 11;16:934834.PMID:35898651DOI:PMC9309612
Risky decision-making is the decision made by individuals when they know the probability of each outcome. In order to survive in unpredictable environments, it is necessary for individuals to assess the probability of events occurring to an make appropriate decisions. There are few studies on the neural basis of risky decision-making behavior guided by external cues, which is related to the relative paucity of animal behavioral paradigms. Previous studies have shown that the prefrontal cortex (PFC) plays a key role in risk-based decision-making. The PFC receives projections from the dopamine (DA) system from the ventral tegmental area of the midbrain. The mesocorticolimbic DA system regulates the judgments of reward and value in decision-making. However, the specific receptor mechanism for prefrontal DA regulation of cue-guided risky decision-making behavior remains unclear. Here we established a cue-guided risky decision-making behavioral paradigm (RDM task) to detect the behavior of rats making decisions between a small certain reward and a large uncertain reward in a self-paced manner. The D1 receptor antagonist SCH-23390 (5 mM) or agonist SKF-82958 (5 mM), and the D2 receptor antagonist thioridazine hydrochloride (5 mM) or agonist MLS-1547 (5 mM) was injected into the mPFC, respectively, to investigate how the behavior in the RDM task was changed. The results showed that: (1) rats were able to master the operation of the cue-guided RDM task in a self-paced way; (2) a majority of rats were inclined to choose risk rather than a safe option when the reward expectations were equal; and (3) risk selection was reduced upon inhibition of D1 receptors or stimulation of D2 receptors, but increased upon stimulation of D1 receptors or inhibition of D2 receptors, suggesting that the RDM performance is regulated by D1 and D2 receptors in the mPFC. The present results suggest that DA receptors in the mPFC of rats are involved in regulating cue-guided RDM behavior, with differential involvement of D1 and D2 receptors in the regulation.