title: Antinociceptive activity of furan-containing congeners of improgan and ranitidine.
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.
authors.affiliation: Center for Neuropharmacology and Neuroscience, Albany Medical College MC-136, Albany, NY 12208, USA. houghl@mail.amc.edu
authors.forename: L B
authors.initials: LB
authors.lastname: Hough
authors.forename: W M P B
authors.initials: WM
authors.lastname: Menge
authors.forename: A C
authors.initials: AC
authors.lastname: van de Stolpe
authors.forename: J W
authors.initials: JW
authors.lastname: Nalwalk
authors.forename: R
authors.initials: R
authors.lastname: Leurs
authors.forename: I J P
authors.initials: IJ
authors.lastname: de Esch
mesh_terms: D000818:Animals; D002927:Cimetidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D005663:Furans / Q000737:chemistry*; D008297:Male; D015394:Molecular Structure; D009619:Nociceptors / Q000378:metabolism*; D011899:Ranitidine / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D005663:Furans; C099531:SKF 92374; D002927:Cimetidine; D011899:Ranitidine; C039281:furan