- 英文名称
- 8-OH-DPAT
- 分子式
- C16H25NO
- 分子量
- 247.38
- 中文别名
- 8-OH-DPAT游离态; 化合物8-OH-DPAT; 8-羟基四氢萘; 8-Oh-dpat; 8-Hydroxy-2-(di-n-propylamino)tetralin; 2-(Dipropylamino)tetralin-8-ol; 2-(N,N-Dipropylamino)-1,2,3,4-tetrahydronaphthalen-8-ol; 5,6,7,8-Tetrahydro-7-(dipropylamino)naphthalen-1-ol; 8-Hydroxy-2-(dipropylamino)-1,2,3,4-tetrahydronaphthalene; 7-(Dipropylamino)-5,6,7,8-tetrahydro-1-naphthalenol; (±)-7-Dipropylamino-5,6,7,8-tetrahydro-naphthalen-1-ol; 7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol; (±)-8-hydroxy-2-(di-N-propylamino)tetralin; 8-HYDROXY-DPAT; (R,S) 7-Dipropylamino-5,6,7,8-tetrahydro-naphthalen-1-ol
- 用途
- - 生物活性
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 466 nM，对 5-HT1B (pIC50, 5.42) 和 5-HT (pIC50 <5) 的作用很弱。
- 靶点
5-HT
1A
Receptor
8.19 (pIC
50
)
5-HT
7
Receptor
466 nM (Ki)
- 体外研究
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC
50
of 8.19 for 5-HT1A; weakly binds to 5-HT1B (pIC
50
, 5.42), 5-HT (pIC
50
<5). 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.
- 体内研究
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.
