GSK1521498 is a potent and selective μ-opioid receptor antagonist. GSK1521498 dose-dependently reduced both cue-controlled alcohol seeking and alcohol intake in the instrumental context as well as alcohol intake in the choice procedure.
|Solubility (25°C)||DMSO ≥ 6 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Tamzin L Ripley, et al. Psychopharmacology (Berl). The novel mu-opioid antagonist, GSK1521498, reduces ethanol consumption in C57BL/6J mice
 Eamonn Kelly, et al. Psychopharmacology (Berl). The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours
 Hisham Ziauddeen, et al. J Clin Pharmacol. The effects of alcohol on the pharmacokinetics and pharmacodynamics of the selective mu-opioid receptor antagonist GSK1521498 in healthy subjects
 Pradeep J Nathan, et al. J Clin Pharmacol. Multiple-dose safety, pharmacokinetics, and pharmacodynamics of the μ-opioid receptor inverse agonist GSK1521498
 Diane M Ignar, et al. J Pharmacol Exp Ther. Regulation of ingestive behaviors in the rat by GSK1521498, a novel micro-opioid receptor-selective inverse agonist
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