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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Zygmunt, Malgorzata Golembiowska, Krystyna Drabczynska, Anna Kiec-Kononowicz, Katarzyna Sapa, Jacek |
| Description | Author Affiliation: Zygmunt M ( Department of Pharmacological Screening, Chair of Pharmacodynamics, Jagiellonian University, Medical College, 9 Medyczna Street, PL 30-688 Krakow, Poland. Electronic address: gogol67@interia.pl.); Golembiowska K ( Department of Pharmacology, Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland); Drabczynska A ( Department of Technology and Biotechnology of Drugs, Jagiellonian University, Medical College, 9 Medyczna Street, PL 30-688 Krakow, Poland.); Kiec-Kononowicz K ( Department of Technology and Biotechnology of Drugs, Jagiellonian University, Medical College, 9 Medyczna Street, PL 30-688 Krakow, Poland.); Sapa J ( Department of Pharmacological Screening, Chair of Pharmacodynamics, Jagiellonian University, Medical College, 9 Medyczna Street, PL 30-688 Krakow, Poland.) |
| Abstract | The purpose of the study was to examine derivatives of annelated xanthines (imidazo-, pyrimido-, and diazepino-purinediones) for potential anti-inflammatory effects in carrageenan-induced paw edema in mice. Additionally, their antioxidant activity using the FRAP (ferric-reducing ability of plasma) assay and lipid peroxidation in rat brain homogenate were analyzed. All the studied derivatives showed affinity for adenosine A receptor. The preliminary assays found that five (KD-114, KD-57, KD-129, KD-50, and KD-358) pyrimidopurinedione derivatives, administered intraperitoneally (i.p.) at a dose of 100mg/kg, had stronger anti-inflammatory effects. At a concentration of 10 M, three of the derivatives KD-57, KD-114, and KD-129 most influenced the total antioxidant ability. The most efficient anti-inflammatory compound, KD-114, also showed the strongest binding to A receptors and when administered at a dose of 5mg/kg (i.p.), effectively reversed haloperidol-induced catalepsy and significantly increased the striatal extracellular dopamine level in the rat striatum. This effect was weaker than the one produced by CSC (1mg/kg i.p.), and only slightly weaker than that produced by ZM 241385 (3mg/kg i.p.) used as reference drugs. From the results of the present studies, it may be concluded that anti-inflammatory and antiparkinsonian effects of the examined compounds correlate with their influence on adenosine A receptors, the most probable antagonism to these subtype receptors. |
| File Format | HTM / HTML |
| ISSN | 00913057 |
| Journal | Pharmacology Biochemistry and Behavior |
| Volume Number | 132 |
| e-ISSN | 18735177 |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2015-02-28 |
| Publisher Place | United States |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Behavioral Sciences Discipline Biochemistry Discipline Pharmacology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Biological Psychiatry Behavioral Neuroscience Biochemistry Clinical Biochemistry Toxicology Pharmacology |
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