Literature DB >> 15013015

4-Substituted anilides as selective melatonin MT2 receptor agonists.

James R Epperson1, Jeffrey A Deskus, Anthony J Gentile, Lawrence G Iben, Elaine Ryan, Nathan S Sarbin.   

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.

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Year:  2004        PMID: 15013015     DOI: 10.1016/j.bmcl.2003.11.030

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Synthetic melatoninergic ligands: achievements and prospects.

Authors:  N V Kostiuk; M B Belyakova; D V Leshchenko; V V Zhigulina; M V Miniaev
Journal:  ISRN Biochem       Date:  2014-02-23

2.  N-(Anilinoethyl)amide Melatonergic Ligands with Improved Water Solubility and Metabolic Stability.

Authors:  Francesca Ferlenghi; Michele Mari; Gabriella Gobbi; Gian Marco Elisi; Marco Mor; Silvia Rivara; Federica Vacondio; Silvia Bartolucci; Annalida Bedini; Fabiola Fanini; Gilberto Spadoni
Journal:  ChemMedChem       Date:  2021-07-26       Impact factor: 3.466

  2 in total

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