2. Academic Validation
  3. A new family of H3 receptor antagonists based on the natural product Conessine

A new family of H3 receptor antagonists based on the natural product Conessine

  • Bioorg Med Chem Lett. 2008 Feb 15;18(4):1490-4. doi: 10.1016/j.bmcl.2007.12.059.
Vincent J Santora 1,  Jonathan A Covel,  Rena Hayashi,  Brian J Hofilena,  Jason B Ibarra,  Michelle D Pulley,  Michael I Weinhouse,  Dipanjan Sengupta,  Jonathan J Duffield,  Graeme Semple,  Robert R Webb,  Carleton Sage,  Albert Ren,  Guilherme Pereira,  Jens Knudsen,  Jeffrey E Edwards,  Marissa Suarez,  John Frazer,  William Thomsen,  Erin Hauser,  Kevin Whelan,  Andrew J Grottick
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA.
PMID: 18194865 DOI: 10.1016/j.bmcl.2007.12.059
Abstract

A new family of Histamine H(3) receptor antagonists (5a-t) has been prepared based on the structure of the natural product Conessine, a known H(3) antagonist. Several members of the new series are highly potent and selective binders of rat and human H(3) receptors and display inverse agonism at the human H(3) receptor. Compound 5n exhibited promising rat pharmacokinetic properties and demonstrated functional antagonism of the H(3) receptor in an in-vivo pharmacological model.

Figures
Products