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Title: The search for selective alfa1A and/or alfa1D-blockers among arylpiperazine derivatives of phenytoin

Abstract:

The aim of this PhD thesis was to determine the activity of nine arylpiperazine derivatives of phenytoin (LL-1, LL-2, LL-3, LL-4, LL-9, BS-8, MN-1, MN-6 and TN-11) toward α1-adrenoceptor subtypes in terms of potential circulatory and urological activity with respect to the reference compounds, and also to investigate the relationship between the structure and affinity for α1-adrenoceptors and pharmacological activity of tested compounds. The results of pharmacological in vivo and in vitro studies showed significant α1-adrenolythic and circulatory activity of tested compounds. None of the tested compounds showed selective α1A- and/or α1D-adrenolytic activity, and therefore none of them have selective affinity for urogenital tract, which could be used in the treatment of benign prostatic hyperplasia.These results showed also a high correlation between the affinity for α1-adrenoceptor of tested compounds and their hypotensive and antiarrhythmic activity, wherein, according to the structure - activity analysis, the highest affinity for α1-adrenoceptors and also the highest α1-adrenolythic activity showed compounds with 2-alkyloxyphenylpiperazine and 3-alkyloxyphenylpiperazine moiety in their structure.

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmakologia ; urologia ; choroby układu krążenia

Degree grantor:

Uniwersytet Jagielloński. Collegium Medicum. Wydział Farmaceutyczny. Katedra Farmakodynamiki.

Promoter:

Barbara Filipek

Date issued:

2014

Format:

application/pdf

Identifier:

oai:dl.cm-uj.krakow.pl:3920 ; farmakologia

Call number:

ZB-121432

ControlNumberVIRTUA:

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Language:

pol

Access rights:

tylko w bibliotece

Location of original object:

Biblioteka Medyczna Uniwersytetu Jagiellońskiego- Collegium Medicum

Object collections:

Last modified:

Sep 17, 2015

In our library since:

Nov 25, 2014

Number of object content hits:

30

Number of object content views in PDF format

30

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/3920

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ZB-121432 Sep 17, 2015
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