LY3154207 (Mevidalen, LY-3154207) is a potent, and subtype selective human dopamine D1 positive allosteric modulator (PAM) with EC50 of 3.0 nM.
LY3154207 displays exquisite selectivity over the human D5 receptor subtype (EC50>10 uM), and 14 other GPCRs, including D2, β1, β2, and 5HT6 receptors.
Mevidalen enhanced wakefulness (latency to fall asleep) in the hD1 mouse in a dose dependent [3-100 mg/kg, orally (PO)] fashion.
Mevidalen promoted wakefulness in mice after prior sleep deprivation and delayed sleep onset by 5.5- and 15.2-fold compared with vehicle-treated animals.
Mevidalen demonstrated a dose-dependent increase in latency to sleep onset in human clinical investigations.
