Synthesis and Analgesic Activity of Annelated Xanthine Derivatives in Experimental Models in Rodents

被引：4

作者：

Zygmunt, Malgorzata ^{[1
]}

Sapa, Jacek ^{[1
]}

Drabczynska, Anna ^{[2
]}

Karcz, Tadeusz ^{[2
]}

Mueller, Christa ^{[3
]}

Koese, Meryem ^{[3
]}

Latacz, Gniewomir ^{[2
]}

Schabikowski, Jakub ^{[2
]}

Bednarski, Marek ^{[1
]}

Kiec-Kononowicz, Katarzyna ^{[2
]}

机构：

[1] Jagiellonian Univ, Coll Med, Dept Pharmacol Screening, PL-30688 Krakow, Poland

[2] Jagiellonian Univ, Coll Med, Dept Technol & Biotechnol Drugs, PL-30688 Krakow, Poland

[3] Univ Bonn, Inst Pharmaceut, PharmaCtr Bonn, Bonn, Germany

来源：

ARCHIV DER PHARMAZIE | 2015年 / 348卷 / 10期

关键词：

Adenosine receptors; Analgesic activity; Pyrimido[2,1-f]purinediones; Xanthines;

D O I：

10.1002/ardp.201500169

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 ED50 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.

引用

页码：704 / 714

页数：11

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