201. Antinociceptive activity of furan-containing congeners of improgan and ranitidine
- Author
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I.J.P. de Esch, Lindsay B. Hough, Wiro M. P. B. Menge, A. C. Van De Stolpe, Julia W. Nalwalk, Rob Leurs, and Medicinal chemistry
- Subjects
Male ,Tertiary amine ,Stereochemistry ,medicine.drug_class ,Clinical Biochemistry ,Analgesic ,Pharmaceutical Science ,Ranitidine ,Biochemistry ,Article ,Rats, Sprague-Dawley ,Structure-Activity Relationship ,Histamine H2 receptor ,Drug Discovery ,medicine ,Animals ,Potency ,Cimetidine ,Furans ,Molecular Biology ,Molecular Structure ,Chemistry ,Organic Chemistry ,Antagonist ,Nociceptors ,Receptor antagonist ,Rats ,Molecular Medicine ,medicine.drug - 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.
- Published
- 2007