Drug intelligence / Profile preview

5-methoxytryptamine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

5-methoxytryptamine, also known as mexamine, is an endogenous indoleamine and a metabolic analog of serotonin and melatonin. It acts as a non-selective agonist at several serotonin receptors, particularly the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 subtypes. Historically, it was utilized as a radioprotective agent (under the name mexamine) due to its ability to induce local hypoxia in hematopoietic tissues. Current clinical and biochemical research focuses on its role as a metabolite and biomarker; for instance, it has been identified as a significant metabolic marker for predicting the risk of recurrent gout flares. Additionally, 5-methoxytryptamine exhibits antioxidant properties, binds to DNA via intercalation, and demonstrates inhibitory activity against both acetylcholinesterase and butyrylcholinesterase. It is also a key substrate in the biosynthetic pathway of melatonin, where it is acetylated by enzymes like arylalkylamine N-acetyltransferase.

Brand names
Mexamine
Other names
Mexamine5-MT5-Methoxytryptamine5-MOTMexaminum
02

Targets

HTR6 (5-hydroxytryptamine receptor 6)HTR4 (5-Hydroxytryptamine receptor 4)HTR7 (5-hydroxytryptamine receptor 7)HTR1D (5-hydroxytryptamine receptor 1D)HTR1B (5-Hydroxytryptamine Receptor 1B)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)

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