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Synthesis and Analgesic Activity of Annelated Xanthine Derivatives in Experimental Models in Rodents
Author(s) -
Zygmunt Małgorzata,
Sapa Jacek,
Drabczyńska Anna,
Karcz Tadeusz,
Müller Christa,
Köse Meryem,
Latacz Gniewomir,
Schabikowski Jakub,
Bednarski Marek,
KiećKoowicz Katarzyna
Publication year - 2015
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201500169
Subject(s) - xanthine , analgesic , chemistry , ed50 , hot plate , pharmacology , biological activity , hot plate test , agonistic behaviour , stereochemistry , receptor , biochemistry , in vitro , enzyme , nociception , medicine , mechanical engineering , psychiatry , engineering , aggression
A series of annelated derivatives of xanthine were synthesized and assayed as potential analgesic agents. All synthesized xanthine derivatives were tested in the writhing test and hot‐plate test. The pharmacological assays demonstrated that all the compounds prepared, without exception, displayed a significant activity in the mouse writhing assay. The analgesic action of the most active compounds, expressed as ED 50 was found to be 1.4–4.3 times more potent than that of acetylsalicylic acid used as the reference compound. However, only some of the compounds demonstrated analgesic activity in the hot‐plate test. The analgesic effect of some compounds is probably related to their agonistic, antagonistic, or partial agonistic activity at the adenosine receptors.