Title: Evaluation of new compounds with α1 adrenolytic activity in experimental models of hypertension


The aim of this doctoral study was evaluation of hypotensive and pleiotropic activity of tested compounds after chronic administration in the selected experimental models of hypertension. Seven compounds with α1-adrenolytic activity were selected for tests, three of which were xanthone derivatives (MH-2, MH-3 and MH-99) and others four were pyrrolidin-2-one derivatives (EP-46, EP-47, EP-49 and EP-58). The main aim of this study required validation of four different animal models of hypertension: DEX model, DOCA model, FRU model and L-NAME model. This last one – L-NAME model – met all assumptions of this study and was selected to evaluation of potential pleiotropic activities of tested compounds. All of tested compounds were evaluated in L-NAME model after chronic administration in terms of their potential hypotensive activity, influence on relaxation of isolated rat-aorta, on glucose and lipid plasma levels, on oxidative stress parameters, on NO2- and NO3- plasma levels, and also on two circulatory biomarker plasma levels – ADMA and VEGF. At the end intrinsic activity for tested compounds towards human α1A-, α1B- and α1D-adrenoceptors was also evaluated. Compounds marked with symbols MH-2, MH-3 and MH-99 showed high therapeutic activity in all pharmacological and biochemical studies. Additionally, these compounds showed also high preferential α1D-adrenolytic activity. These results suggest that α1D-adrenolytic activity of tested compound may be connected with their hypotensive activity and with their corrective influence on disturbed endothelium function induced in L-NAME hypertension model.

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Level of degree:

2 - studia doktoranckie

Degree discipline:

choroby układu krążenia

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Uniwersytet Jagielloński. Collegium Medicum. Wydział Farmaceutyczny. Zakład Wstępnych Badań Farmakologicznych Katedry Farmakodynamiki.


Jacek Sapa ; Marek Bednarski

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Biblioteka Medyczna Uniwersytetu Jagiellońskiego- Collegium Medicum

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May 10, 2019

In our library since:

May 6, 2019

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Edition name Date
ZB-127565 May 10, 2019


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