4-Substituted anilides as selective melatonin MT2 receptor agonists.
Article Details
- CitationCopy to clipboard
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]
- 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