Antinociceptive activity of furan-containing congeners of improgan and ranitidine.
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.
Hough
L B
LB
Center for Neuropharmacology and Neuroscience, Albany Medical College MC-136, Albany, NY 12208, USA. houghl@mail.amc.edu
Menge
W M P B
WM
van de Stolpe
A C
AC
Nalwalk
J W
JW
Leurs
R
R
de Esch
I J P
IJ
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
D005663:Furans; C099531:SKF 92374; D002927:Cimetidine; D011899:Ranitidine; C039281:furan