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Antinociceptive activity of furan-containing congeners of improgan and ranitidine.

Hough LB, Menge WM, van de Stolpe AC, Nalwalk JW, Leurs R, de Esch IJ

Center for Neuropharmacology and Neuroscience, Albany Medical College MC-136, Albany, NY 12208, USA. houghl@mail.amc.edu

Furan-containing congeners of the histamine H(2) receptor antagonist ranitidine were synthesized and tested for improgan-like antinociceptive activity. The most potent ligand of the series, VUF5498, is the most potent improgan-like agent described to date (ED(50)=25 nmol, icv). This compound is approximately equal in potency with morphine. These non-imidazole, improgan-like pain relievers further define the structural requirements for analgesics of this class and are important tools for ongoing mechanism-based studies.

Published 18 September 2007 in Bioorg Med Chem Lett, 17(20): 5715-9.
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