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

Autor: Hough LB; Center for Neuropharmacology and Neuroscience, Albany Medical College MC-136, Albany, NY 12208, USA. houghl@mail.amc.edu, Menge WM, van de Stolpe AC, Nalwalk JW, Leurs R, de Esch IJ
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Oct 15; Vol. 17 (20), pp. 5715-9. Date of Electronic Publication: 2007 Aug 19.
DOI: 10.1016/j.bmcl.2007.07.060
Abstrakt: 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.
Databáze: MEDLINE