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

Author:

Mogilski, Szczepan

Date:

2012

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:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmakologia

Degree grantor:

Wydział Farmaceutyczny

Promoter:

Filipek, Barbara

Date issued:

2011

Identifier:

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

Call number:

ZB-116303

Language:

pol

Access rights:

tylko w bibliotece

Subject and keywords:

[3 4-d]pyridazine histamine pain inflammation phosphodiesterase

Object collections:

Last modified:

Mar 17, 2023

In our library since:

Mar 11, 2013

Number of object content hits:

9

Number of object content views in PDF format

0

All available object's versions:

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

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Edition name Date
ZB-116303 Mar 17, 2023

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