PD-168077-maleate - Dopamine Receptor Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPD-168077 maleateCat. No.: HY-21098ACAS No.: 630117-19-0分式: CHNO分量: 450.49作靶点: Dopamine Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg

2、/mL (332.97 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2198 mL 11.0990 mL 22.1981 mL5 mM 0.4440 mL 2.2198 mL 4.4396 mL10 mM 0.2220 mL 1.1099 mL 2.2198 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您

3、现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.55 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.55 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility:

4、 2.5 mg/mL (5.55 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 PD-168077 maleate个选择性的多巴胺 D4 受体激动剂，其 Ki 值为 9 nM。IC50 & Target Ki: 9 nM (Dopamine D4 receptor) 1.体外研究 PD-168077 is one of the first agents to be identified as putative selective D4 agonists. It

5、 shows 100-foldselectivity over other members of the D2-like receptor family and over their D1-like counterparts; PD-168077shows a 20-fold selectivity over 1, and 2, a 45-fold selectivity over 5-HT1A, and a 460-fold selectivity over5-HT2A receptors; PD-168077 evidences intrinsic activity at the D4 r

6、eceptor in terms of quinpirole-likeinhibition of forskolin-stimulated cAMP accumulation or stimulation of 3Hthymidine uptake in CHO cellsexpressing the human D4 receptor 1. In the PD-168077-treated cell, p-CaMKII exhibits a significantlyincreased clustering at synaptic sites, as indicated by the enh

7、anced colocalization with PSD-95 2.体内研究 PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual andcharacteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes ofmyoclonic jerking; grooming, and rearing are reduced 1.REFERENCES1. Cli

8、fford JJ, et al. Topographically based search for an Ethogram among a series of novel D(4) dopamine receptor agonists andantagonists. Neuropsychopharmacology. 2000 May;22(5):538-44.2. Gu Z, et al. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II incultured prefrontal cortical neurons. Mol Pharmacol. 2006 Mar;69(3):813-22.McePdfHeightCaution: Product has not been fully validated for medical applica