Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.
Article Details
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Descamps-Francois C, Yous S, Chavatte P, Audinot V, Bonnaud A, Boutin JA, Delagrange P, Bennejean C, Renard P, Lesieur D
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.
J Med Chem. 2003 Mar 27;46(7):1127-9.
- PubMed ID
- 12646022 [ View in PubMed]
- Abstract
We report the synthesis and binding properties at MT(1) and MT(2) receptors of the first example of agomelatine (N-[2-(7-methoxynaphth-1-yl)ethyl]acetamide) dimers in which two agomelatine moieties are linked together through their methoxy substituent by a polymethylene side chain according to the "bivalent ligand" approach. Some of these compounds behave as MT(1)-selective ligands. The most selective one (5) behaves as an antagonist.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Agomelatine Melatonin receptor type 1A Ki (nM) 0.06 N/A N/A Details Agomelatine Melatonin receptor type 1A EC 50 (nM) 1.56 N/A N/A Details Agomelatine Melatonin receptor type 1B EC 50 (nM) 0.1 N/A N/A Details Agomelatine Melatonin receptor type 1B Ki (nM) 0.27 N/A N/A Details Melatonin Melatonin receptor type 1A EC 50 (nM) 2.24 N/A N/A Details Melatonin Melatonin receptor type 1A Ki (nM) 0.14 N/A N/A Details Melatonin Melatonin receptor type 1B EC 50 (nM) 0.49 N/A N/A Details Melatonin Melatonin receptor type 1B Ki (nM) 0.41 N/A N/A Details