| Literature DB >> 18194865 |
Vincent J Santora1, 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.
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.Entities:
Mesh：
Substances：
Year: 2007 PMID： 18194865 DOI： 10.1016/j.bmcl.2007.12.059
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823