Analgesic activity of selected [3,4-d] pyridazine derivatives - Digital Medical Library

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Title: Analgesic activity of selected [3,4-d] pyridazine derivatives

Author:

Mogilski, Szczepan

Date:

Type:

Praca doktorska

Abstract:

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.

Place of publishing:

Level of degree:

2 - studia doktoranckie

Degree grantor:

Wydział Farmaceutyczny

Promoter:

Filipek, Barbara

Date issued:

Identifier:

oai:dl.cm-uj.krakow.pl:3480

Call number:

Language:

Access rights:

tylko w bibliotece

Subject and keywords:

[3,4-d]pyridazine, histamine, pain, inflammation, phosphodiesterase

Object collections:

Digital Medical Library > PhD thesis database

Last modified:

Feb 18, 2022

In our library since:

Mar 11, 2013

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9

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All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/3480

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Edition name	Date
ZB-116303	Feb 18, 2022

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Analgesic activity of selected [3,4-d] pyridazine derivatives

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2012

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