2. Academic Validation
  3. Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model

Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model

  • J Med Chem. 2004 Mar 25;47(7):1602-4. doi: 10.1021/jm034244g.
Tricia J Vos 1,  Andrei Caracoti,  Jennifer L Che,  Mingshi Dai,  Cheryl A Farrer,  Nancy E Forsyth,  Stacey V Drabic,  Robert A Horlick,  Diana Lamppu,  David L Yowe,  Suresh Balani,  Ping Li,  Hang Zeng,  Ingrid B J K Joseph,  Luis E Rodriguez,  Martin P Maguire,  Michael A Patane,  Christopher F Claiborne
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Millennium Pharmaceuticals, Inc., 40 Landsdowne Street, Cambridge, Massachusetts 02139, USA. tricia.vos@mpi.com
PMID: 15027849 DOI: 10.1021/jm034244g
Abstract

The melanocortin 4 receptor (MC4R) plays an important role in body weight regulation and energy homeostasis. Administration of peptidic MC4R antagonists (usually by intracerebro ventricular injection) has been shown in the literature to increase body weight and/or food intake in several rodent models. We report here the identification of a novel nonpeptidic MC4R Antagonist and its effects on tumor-induced weight loss in mice following peripheral administration.

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