Drug intelligence / Profile preview

2-iodomelatonin

Development stage
Unknown
Modality
Small Molecules
01

Overview

**2-Iodomelatonin** is a synthetic analog of melatonin, structurally characterized as an iodinated derivative of the natural hormone. It acts as a potent and selective agonist at melatonin receptors, particularly showing high affinity for the melatonin receptor type 1 (MT1), with approximately fivefold selectivity over the MT2 subtype. Its primary use is experimental, serving as a radioligand or pharmacological tool to study melatonergic signaling pathways and receptor pharmacology in vitro and in vivo. It has not been approved for therapeutic use in humans[9]. Mechanistically, it inhibits forskolin-stimulated cAMP production via activation of MT1 receptors much more potently than endogenous melatonin[9].

Other names
N-[2-(2-iodo-5-methoxy-1H-indol-3-yl)ethyl]acetamideN-(2-(2-Iodo-5-methoxyindol-3yl)ethyl)acetamideN-Acetyl-2-iodo-5-methoxytryptamineN-Acetyl2-iodo-5-methoxytryptamineN-Acetyl 2-iodo-5-methoxytryptamineAcetamide, N-[2-(2-Iodo–5-methoxy–1H-indol–3–yl)ethyl]-
02

Targets

MTNR1A (MT1)MTNR1B (Melatonin Receptor 2)

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