@misc{Nowiński_Leszek_The_2014, author={Nowiński, Leszek}, address={Kraków}, howpublished={online}, year={2014}, school={Wydział Farmaceutyczny}, language={pol}, 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.}, title={The search for selective alfa1A and/or alfa1D-blockers among arylpiperazine derivatives of phenytoin}, type={Praca doktorska}, keywords={arrhythmia, prostate, alfa1-blockers, hipertension, urogenital}, }