GSK598809 - Dopamine Receptor Antagonist - 生命科學(xué)試劑 - 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 : 83.33 mg/mL (

2、173.06 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)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(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)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?，配制前?qǐng)先配制澄清的儲(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，建議您現(xiàn)現(xiàn)配，當(dāng)

3、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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.32 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.32 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.

4、08 mg/mL (4.32 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK598809是多巴胺 D3 受體 (DRD3) 的選擇性拮抗劑，其pKi 值為 8.9。IC50 & Target pKi: DRD3 1 2.體內(nèi)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