PD-168077-maleate - Dopamine Receptor Agonist - 生命科學(xué)試劑 - 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作靶點(diǎn): Dopamine Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 150 mg

2、/mL (332.97 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬?chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您

3、現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.55 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.55 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility:

4、 2.5 mg/mL (5.55 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 PD-168077 maleate個(gè)選擇性的多巴胺 D4 受體激動(dòng)劑，其 Ki 值為 9 nM。IC50 & Target Ki: 9 nM (Dopamine D4 receptor) 1.體外研究 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.體內(nèi)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