GSK598809 - Dopamine Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK598809Cat. No.: HY-19654CAS No.: 863680-45-9分式: CHFNOS分量: 481.51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 : 83.33 mg/mL (

2、173.06 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0768 mL 10.3840 mL 20.7680 mL5 mM 0.4154 mL 2.0768 mL 4.1536 mL10 mM 0.2077 mL 1.0384 mL 2.0768 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，建议您现现配，当

3、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: 2.08 mg/mL (4.32 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.32 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.

4、08 mg/mL (4.32 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK598809是多巴胺 D3 受体 (DRD3) 的选择性拮抗剂，其pKi 值为 8.9。IC50 & Target pKi: DRD3 1 2.体内研究 Cocaine and GSK598809 each increases peak mean arterial blood pressure. Least square mean differencesare significa

5、nt for both doses of cocaine compared with its vehicle. Likewise, least square mean differencesare significant for both doses of GSK598809 as compared with its vehicle. The experimental question ofinterest, that is, whether GSK598809 significantly increases cocaine effects on peak mean arterial bloo

6、dpressure, is probed by a prior it tests on the means of the fitted regression model. The dose of 3 mg/kgGSK598809 significantly increases the pressor effects of 5.6 mg/kg cocaine and of 1.7 mg/kg cocaine 1.PROTOCOLAnimal Dogs 1Administration 1 Male beagle dogs are used throughout the study. The exp

7、eriment is conducted in phases. In the first(hemodynamics) phase, the dogs are dosed at weekly intervals over a period of 9 weeks with combinationsof either GSK598809 or vehicle, followed by either cocaine or vehicle. After the baseline measurements arerecorded, technical staff briefly returns to th

8、e animal room to administer GSK598809 (or vehicle) to all thedogs via oral gavage and activate the timers on the preloaded and preprogrammed infusion pumps 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Appel NM, et al. Dopamine D3 Recep

9、tor Antagonist (GSK598809) Potentiates the Hypertensive Effects of Cocaine in Conscious, Freely-Moving Dogs. J Pharmacol Exp Ther. 2015 Sep;354(3):484-92.2. Micheli F, et al. 1,2,4-Triazolyl azabicyclo3.1.0hexanes: a new series of potent and selective dopamine D(3) receptor antagonists. JMed Chem. 2010 Jan 14;53(1):374-91.McePdfHeightCaution: Product has not been fully validated for medi