GSK598809

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK598809 (GSK-598809) 是一种有效、选择性、中枢神经系统渗透性、口服生物可利用的多巴胺 D3 受体拮抗剂，pKi 为 8.9；显示出比 D2 和 H1 受体高 100 倍的选择性。

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9; displays >100-fold selectivity over D2 and H1 receptors; significantly attenuates the expression of conditioned place preference (CPP) to nicotine and cocaine; potentiates the hemodynamic effects of cocaine in dogs, also increases mean arterial blood pressure and heart rate in vivo.

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Cocaine and GSK598809 each increases peak mean arterial blood pressure. Least square mean differences are significant for both doses of cocaine compared with its vehicle. Likewise, least square mean differences are significant for both doses of GSK598809 as compared with its vehicle. The experimental question of interest, that is, whether GSK598809 significantly increases cocaine effects on peak mean arterial blood pressure, is probed by a prior it tests on the means of the fitted regression model. The dose of 3 mg/kg GSK598809 significantly increases the pressor effects of 5.6 mg/kg cocaine and of 1.7 mg/kg cocaine.

GSK 598809 | GSK-598809

GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

Other Indications

Other Disease

863680-45-9

481.514

C22H23F4N5OS

>98% (HPLC)

DMSO : 83.33 mg/mL 173.06 mM

CC1=C(OC=N1)C2=NN=C(N2C)SCCCN3CC4CC4(C3)C5=C(C=C(C=C5)C(F)(F)F)F

1-[2-Fluoro-4-(trifluoromethyl)phenyl]-3-[3-[[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio]propyl]-3-azabicyclo[3.1.0]hexane

(-20℃)

With Ice Pack

≥ 2 years