Antinociceptive activity of furan-containing congeners of improgan and ranitidine

Authors :: I.J.P. de Esch
Lindsay B. Hough
Wiro M. P. B. Menge
A. C. Van De Stolpe
Julia W. Nalwalk
Rob Leurs
Medicinal chemistry
Source :: Hough, L H, Menge, W M P B, van de Stolpe, A, Nalwalk, J B, Leurs, R & de Esch, I J P 2007, ' Antinociceptive activity of furan-containing congeners of improgan and ranitidine ', Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 20, pp. 5715-9 . https://doi.org/10.1016/j.bmcl.2007.07.060, Bioorganic and Medicinal Chemistry Letters, 17(20), 5715-9. Elsevier Limited
Publication Year :: 2007
Publisher :: Elsevier Limited, 2007.
Abstract: 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.

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