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A new family of H3 receptor antagonists based on the natural product Conessine |
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| Authors: | Santora Vincent J Covel Jonathan A Hayashi Rena Hofilena Brian J Ibarra Jason B Pulley Michelle D Weinhouse Michael I Sengupta Dipanjan Duffield Jonathan J Semple Graeme Webb Robert R Sage Carleton Ren Albert Pereira Guilherme Knudsen Jens Edwards Jeffrey E Suarez Marissa Frazer John Thomsen William Hauser Erin Whelan Kevin Grottick Andrew J |
| Affiliation: | Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. |
| 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. |
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