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Novel imidazole-based histamine H3 antagonists |
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| Authors: | Jill A Jablonowski Kiev S Ly Michael Bogenstaetter Curt A Dvorak Jamin D Boggs Lisa K Dvorak Brian Lord Kirsten L Miller Curt Mazur Sandy J Wilson Timothy W Lovenberg Nicholas I Carruthers |
| Institution: | Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA |
| Abstract: | A novel series of imidazole containing histamine H3 receptor ligands were investigated and found to be potent functional antagonists. After improving the stability of these molecules towards liver microsomes, these compounds were found to have no appreciable affinity for CYP P450s. Subsequent in vivo experiments showed significant brain uptake of (4-chloro-phenyl)-2-(1-isopropyl-piperidin-4-ylmethoxy)-3-methyl-3H-imidazol-4-yl]-methanone 22. |
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