Obiekt
Tytuł: Pharmacological evaluation of the central, local anaesthetic and haemodynamic activity of new chiral aminobutanol derivatives of xanthone
Abstrakt:
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.
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Data ostatniej modyfikacji:
28 lut 2023
Data dodania obiektu:
21 lis 2012
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http://dl.cm-uj.krakow.pl:8080/publication/1102
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| Nazwa wydania | Data |
|---|---|
| ZB-105381 | 28 lut 2023 |
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