8-OH-DPAT是一种有效的，选择性的5-HT激动剂，对5-HT1A的pIC50值为8.19，对5-HT7的Ki值为466nM，对5-HT1B(pIC50,5.42)和5-HT(pIC50<5)的作用很弱。
CAS：78950-78-4
分子式：C16H25NO
分子量：247.38
纯度：98%
存储：Store at -20°C

Background:

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

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 Ki of 466 nM, and does not bind to 5-HT6 or 5-HT4[2].

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].

[1]. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF [2]. Bard JA, et al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. [3]. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT. Psychopharmacology (Berl). 2016 Jun;233(12):2343-53.