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Title: Pharmacological evaluation of the central, local anaesthetic and haemodynamic activity of new chiral aminobutanol derivatives of xanthone

Abstract:

The purpose of the present work was the pharmacological evaluation of the central, local anaesthetic and haemodynamic activity of 9 new chiral aminobutanol derivatives of xanthone. Moreover, also the differences in pharmacological activity between enantiomers of these chiral compounds were investigated. The compounds were examined in models of epilepsy (MES test, pentylentetrazole and picrotoxin induced seizures) and their influence on spontaneous locomotor activity, in Porsolt and in chimney test. The more potent antiepileptic effects were observed for compound MH2 and especially for its enantiomer R. The local anaesthetic (LA) activity was examined in animal models of LA (corneal and infiltration anaesthesia). All these compounds, especially enantiomers R, shown higher than mepiwacine, LA properties. The influence on circulation activity was evaluated in: the blood pressure of normotensive rats and models of arrhythmias (adrenaline-, BaCl2- and CaCl2-inducted arrhythmia). All compounds shown low antiarrhythmic activity. Compounds MH20, its enantiomer S and MH2 significantly decreased blood pressure and demonstrated affinity to α adrenoceptors. Antiepileptic activity in MES test, LA activity, the effect on ECG parameters and also some protective effect in BaCl2 induced arrhythmia may suggest membrane stabilizing activity of these investigated compounds. These obtained results demonstrated different strength of enantiomers and racemic mixture in affecting CNS functions, LA and haemodynamic activity, which indicate the importance to pharmacologically examine enantiomers, not only racemic mixtures of newly synthesized compounds.

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmakologia

Degree grantor:

Wydział Farmacji

Promoter:

Ryszard Czarnecki

Date issued:

2006

Format:

application/pdf

Identifier:

oai:dl.cm-uj.krakow.pl:1102

Call number:

ZB-105381

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Access rights:

tylko w bibliotece

Location of original object:

Biblioteka Medyczna Uniwersytetu Jagiellońskiego - Collegium Medicum

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Last modified:

Feb 12, 2020

In our library since:

Nov 21, 2012

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All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/1102

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ZB-105381 Feb 12, 2020
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