tcsc0043224 8-OH-DPAT

8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC₅₀ of 8.19 for 5-HT1A and a K_i of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5).

IC50 & Target: pIC50: 8.19 (5-HT1A)^[1]


Ki: 466 nM (5-HT7)^[2]

In Vitro: 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC₅₀ of 8.19 for 5-HT1A; weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5)^[1]. 8-OH-DPAT has high affinity at 5-HT7 with a K_i of 466 nM, and does not bind to 5-HT6 or 5-HT4^[2].

In Vivo: 8-OH-DPAT (1 mg/kg) normalizes hypolocomotion, significantly increases wakefulness and reduces the duration of REM sleep without effect on the duration of non-REM sleep in the dark period in orexin knockout (KO) mice. 8-OH-DPAT shows no obvious effect on wakefulness or the duration of either REM sleep or non-REM sleep in WT mice. 8-OH-DPAT (1 mg/kg, s.c.) activates 5-HT1A receptor in orexin knockout mice^[3].