N-Acetyl-5-hydroxytryptamine (NAS) is the precursor of melatonin, acetylated from serotonin by AANAT (arylalkylamine N-acetyltransferase). N-Acetyl-5-hydroxytryptamine activates TrkB receptors in a circadian rhythm and exerts antidepressant effects in a TrkB-dependent manner. N-Acetyl-5-hydroxytryptamine rapidly activates TrkB, but not TrkA or TrkC, in a neurotrophin-independent and MT3 receptor-independent manner[1] .
To evaluate the activation of TrkB receptor by HIOC, results showed that HIOC significantly activated TrkB receptor and its downstream effector Akt at 500 nM.
Proc Natl Acad Sci U S A. 2012 Feb 28;109(9):3540-5
P1.HTR cells
30 μM
24 hours
To evaluate the effect of NAS on IDO1 catalytic activity, results showed NAS increased Kyn production.
Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3848-3857
dendritic cells
30 μM
24 hours
To evaluate the effect of NAS on IDO1 catalytic activity, results showed NAS significantly increased Kyn release.
Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3848-3857
human epidermal keratinocytes
10−7–10−3 M
24, 48 and 72 hours
To evaluate the effect of N-Acetyl-5-hydroxytryptamine on cell viability, results showed that N-Acetyl-5-hydroxytryptamine affected cell viability at concentrations of 10−7–10−3 M.
J Pineal Res. 2020 Mar;68(2):e12626
human epidermal melanocytes
10−4-10−3 M
72 hours
To evaluate the inhibitory effect of N-Acetyl-5-hydroxytryptamine on melanogenesis, results showed that N-Acetyl-5-hydroxytryptamine significantly inhibited melanogenesis at concentrations of 10−4-10−3 M.
J Pineal Res. 2020 Mar;68(2):e12626
HEK293 cells
1 nM to 100 μM
60 minutes
To evaluate the agonist activity of N-Acetyl-5-hydroxytryptamine (NAS) on human MT1 and MT2 melatonin receptors. Results showed that NAS activates MT1 and MT2 receptors but with lower potency than melatonin.
J Pineal Res. 2020 Mar;68(2):e12622
N-Acetyl-5-hydroxytryptamine 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
TrkB F616A knock-in mice
Intraperitoneal injection
20 mg/kg
Single injection
To evaluate the neuroprotective effects of HIOC in vivo, results showed that HIOC significantly suppressed KA-induced neuronal apoptosis via TrkB receptor activation.
Proc Natl Acad Sci U S A. 2012 Feb 28;109(9):3540-5
Mice
Experimental autoimmune encephalomyelitis (EAE) model
Intraperitoneal injection
10 mg/kg
Every other day for 24 days
To evaluate the protective effect of NAS on EAE, results showed NAS significantly alleviated clinical symptoms and pathological changes of EAE.
Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3848-3857
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