2. Academic Validation
  3. Aminopyrazine CB1 receptor inverse agonists

Aminopyrazine CB1 receptor inverse agonists

  • Bioorg Med Chem Lett. 2008 Jun 1;18(11):3376-81. doi: 10.1016/j.bmcl.2008.04.022.
David J Wustrow 1,  George D Maynard,  Jun Yuan,  He Zhao,  Jianmin Mao,  Qin Guo,  Mark Kershaw,  Jack Hammer,  Robbin M Brodbeck,  Kristen E Near,  Dan Zhou,  David S Beers,  Bertrand L Chenard,  James E Krause,  Alan J Hutchison
Affiliations

Affiliation

  • 1 Neurogen Corporation, 35 Northeast Industrial Road, Branford CT 06405, USA. dwustrow@nrgn.com
PMID: 18448340 DOI: 10.1016/j.bmcl.2008.04.022
Abstract

A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like properties including solubility and Cytochrome-P450 inhibition potential. Optimized compounds were demonstrated to be inverse agonists and compared in vivo with rimonabant for their ability to inhibit food intake, to occupy central CB1 receptors and to influence hormonal markers associated with obesity.

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