Table 1 Comparison of in vitro potency and in vivo wake-promoting effects between TAK-861 and TAK-994. In vitro potency on recombinant hOX2R and the MED for wakefulness in WT mice and cynomolgus monkeys between TAK-861 and TAK-99416,45. EC50 half-maximal effective concentration, hOX[1/2]R human orexin receptor [1/2], MED minimum effective dose, p.o. orally, WT wild type.

From: TAK-861, a potent, orally available orexin receptor 2-selective agonist, produces wakefulness in monkeys and improves narcolepsy-like phenotypes in mouse models

 

TAK-861

TAK-994

In vitro potency (hOX2R EC50)

2.5 nM

19 nM

Selectivity to hOX2R over hOX1R

× 3000

× 740

MEDs for wakefulness in WT animals

 Mice

1 mg/kg, p.o

10 mg/kg, p.o

 Monkeys

1 mg/kg, p.o

10 mg/kg, p.o

Back to article page