4-Substituted anilides as selective melatonin MT2 receptor agonists.

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Epperson JR, Deskus JA, Gentile AJ, Iben LG, Ryan E, Sarbin NS

4-Substituted anilides as selective melatonin MT2 receptor agonists.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1023-6.

PubMed ID

15013015 [ View in PubMed

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Abstract

A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2) binding affinity and MT(2) selectivity of at least 70-fold over the MT(1) receptor. Compound 26 demonstrated full agonism at the MT(2) receptor.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Melatonin receptor type 1A	Ki (nM)	0.53	N/A	N/A	Details
Melatonin	Melatonin receptor type 1B	Ki (nM)	0.32	N/A	N/A	Details