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Mogilski, Szczepan
2012
Praca doktorska
The aim of this study was to evaluate the analgesic activity and additional pharmacological properties of [3,4-d]piridazine derivatives and the explanation of their mechanism of action. On the basis of the results of preliminary studies ('writhing' and 'hot plate' test) seven structures from the group of fifteen compounds were selected for further studies. In these studies, tested compounds showed a significant antinociceptive effect in animal models of pain induced by formalin, capsaicin and glutamic acid. They also demonstrated significant anti-inflammatory activity in carrageenan and zymosan A induced animal models of acute inflammation. Investigated compounds are characterized by a wide therapeutic index. They also proved to be safe in terms of cardiovascular effects (no influence on QTC interval). In subsequent studies, including experiments on isolated organs, radioligand assays, biochemical and behavioral tests, it was demonstrated that analgesic and anti-inflammatory effect of the investigated structures is largely due to their antihistaminic activity, the phosphodiesterase inhibition and additional mechanisms. In the case of the compound TZ 64 the interaction with 5-HT1A receptor is important, whereas for several other compounds weak α-adrenoreceptor blocking properties, weak antagonism to 5-HT3 receptor or antioxidant activity cannot be excluded.
Kraków
2 - studia doktoranckie
Wydział Farmaceutyczny
Filipek, Barbara
2011
oai:dl.cm-uj.krakow.pl:3480
ZB-116303
pol
tylko w bibliotece
Feb 18, 2022
Mar 11, 2013
9
0
http://dl.cm-uj.krakow.pl:8080/publication/3480
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OAI-PMH
Citation style: chicago-author-date iso690-author-date
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