Cabergoline-FCE-21336-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECabergolineCat. No.: HY-15296CAS No.: 81409-90-7Synonyms: FCE-21336分式: CHNO分量: 451.6作靶点: Dopamine Receptor; Autophagy作通路: GPCR/G Protein; Neuronal Signaling; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20

2、C 1 month溶解性数据体外实验 DMSO : 33 mg/mL (73.07 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2143 mL 11.0717 mL 22.1435 mL5 mM 0.4429 mL 2.2143 mL 4.4287 mL10 mM 0.2214 mL 1.1072 mL 2.2143 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物

3、活性 Cabergoline种麦衍的多巴胺 D2 亚类受体激动剂，亲和作于 D2，D3 和 5-HT2B 受体，Ki 分别为 0.7，1.5 和 1.2。IC50 & Target Ki: 0.7 (Dopamine D2 receptor), 1.5 (Dopamine D3 receptor), 1.2 (5-HT2B receptor) 11/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Cabergoline acts as a potent agonist of D2, D3 and 5-HT2B receptors. Pre

4、treatment with Cabergoline inhibitsH2O2-induced neuronal cell death in a dose-dependent manner. In the following experiments, 10 M ofCabergoline is used to investigate its neuroprotective effects. MAP2 staining reveals that Cabergolinesignificantly suppresses the loss of neurons caused by H2O2 incub

5、ation. The detection of apoptotic nuclearcondensation suggested that Cabergoline prevents apoptotic cell death following H2O2 exposure 1.体内研究 Cabergoline has a longer elimination half-life (63 to 109 h) compared with other D2-like receptor agonists,both a long-lasting clinical effect following singl

6、e-dose administration, and an improvement in the quality oflife of patients with chronic diseases are expected 1. The most significant reduction in rapid eye movement(REM) sleep bout number occurred during the light phase, in which Cabergoline-injected female handledmice has 67.3% less REM sleep bou

7、ts (F(1,11)=12.892, P=0.004) than Cabergoline-injected females that arerestrained, although the greatest number in reduction of REM sleep bouts occurr during the dark phase(82.3% fewer REM sleep bouts; F(1,11)=3.667, P=0.082). In male mice, Cabergoline reduces baselineProlactin (PRL) levels (98.5%;

8、F(1,6)=13.192, P=0.011) from 5.81.3 to 0.08 ng/mL within 2 hours ofinjection. After a 7-day recovery period, PRL levels return to values that are not different from baseline(5.00.60 ng/mL; F(1,6)=0.715, P=0.43) 2.PROTOCOLCell Assay 1 Primary cortical neurons are prepared. Cabergoline (10 M; except f

9、or experiments of dose-dependency) isapplied to cortical cells at DIV 6-7. After 24-hour Cabergoline treatment (except for examination ofpretreatment time-dependency of Cabergoline), H2O2 (50 M; except for the dose-dependency of H2O2) isadded. All inhibitors and antagonists, including spiperone, U01

10、26, SB203580, SP600125, AP5, andnifedipine are applied 20 min before Cabergoline or H2O2 addition. L-glutamate is added at DIV 7-8 for celldeath induction. Cell survival rate is measured by MTT assay. After the indicated treatment with drugs iscompleted, culture medium is replaced with 200 L fresh m

11、edium containing 40 l MTT solution (2.5 mg/mL,diluted in PBS) and cells are incubated at 37C for 1.5-2.5 hours. Then, 200 L lysis buffer containingisopropyl alcohol is applied to each well and mixed by pipetting. Each sample is moved to a 96-well plate andits absorbance at 570 nm is measured using a

12、n iMark Micro plate leader. Cell survival rate is quantitated byabsorbance measurement, because MTT (yellow) is deoxidized to formazan (violet) in proportion tomitochondrial activity 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Adminis

13、tration 2 Female and male C57BL/6J mice are used.Cabergoline is dissolved in 100% pharmasolve and then dilutedwith 20% -cyclodextrin in water to yield a final concentration of 0.15-0.5 mg/mL Cabergoline. Mice receiveda 0.3-mg/kg ip injection of Cabergoline or vehicle. All drugs are prepared within 4

14、8 hours of experiment andstored at 4C. Solutions are allowed to reach at room temperature before injection.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Odaka H, et al. Cabergoline, dopamine D2 receptor agonist, prevents neuronal cell death under oxidative stress via reducingexcitotoxicity. PLoS One. 2014 Jun 10;9(6):e99271.2. Jefferson F, et al. A dopamine receptor d2-type agonist attenuates the ability of stress to alter sleep in mice. Endocrinology. 2