N-Acetyl-5-hydroxytryptamine 是褪黑激素的直接前体,能够有效激活TrkB受体。
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N-Acetylserotonin (NAS), also known as Normelatonin, is the immediate precursor of melatonin. It is produced from serotonin by the enzyme aralkylamine N-acetyltransferase and is converted to melatonin by acetylserotonin O-methyltransferase. It can potently activate TrkB receptor.
体外活性
N-acetylserotonin activates TrkB receptor in a circadian rhythm. N-Acetyl-5-hydroxytryptamine swiftly activates TrkB in a circadian manner and exhibits antidepressant effect in a TrkB-dependent manner. N-Acetyl-5-hydroxytryptamine rapidly activates TrkB, but not TrkA or TrkC, in a neurotrophin- and MT3 receptor-independent manner[1].
体内活性
To explore whether N-Acetyl-5-hydroxytryptamine, can trigger TrkB activation in vivo, TrkB F616A knockin mice are employed, where it has been shown that TrkB F616A activation can be selectively blocked by 1NMPP1, a derivative of kinase inhibitor PP1, leading to TrkB-null phenotypes. To assess whether N-Acetyl-5-hydroxytryptamine can mimic BDNF, cortical neurons from TrkB F616A knockin mice are prepared. In alignment with a previous report, BDNF- and NAS-mediated TrkB phosphorylation are selectively reduced by 1NMPP1 but not by K252a, whereas serotonin or Melatonin had no effect. These findings indicate that NAS strongly provokes both wild-type TrkB and TrkB F616A tyrosine phosphorylation and activation[1].
Cas No.
1210-83-9
分子式
C12H14N2O2
分子量
218.256
别名
O-Demethylmelatonin;N-Acetylserotonin;N-乙酰-5-羟色胺;Normelatonin
储存和溶解度
Ethanol:10 mg/mL
DMSO:12 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years