@misc{Zygmunt_Małgorzata_Affinity_2005, author={Zygmunt, Małgorzata}, address={Kraków}, howpublished={online}, year={2005}, school={Wydział Farmaceutyczny}, language={pol}, abstract={Searching for compounds with potential activity on cardiovascular system within the group of 7,8- disubstituted derivatives of theophylline m the Department of Pharmaceutical Chemistry of Collegium Medicum of Jagiellonian University, we obtained new 7-β-hydroxy- γ-(N4phenoxyethylpiperazine)-propyl derivatives. Initial pharmacological studies lead to the selection of 7- β -hydroxy- γ -(N4-phenoxyethylpiperazine)-propyltheophylline dihydrochloride (CH-1), a compound that exhibits an antiarrythmic, hypotensive activity and an affinity for α1, and α2 -adrenergic receptors. As a result of a modification of the compound CH-1 consisting in the introduction of vanous arylalkylamino or aminoalkylamino substituents at the 8-position of theophylline, as well as, by substituting phenoxyethylpiperazine by another piperazine group, seven active structures were obtained that exhibited comparable or higher antiarrythmic and/or hypotensive effect and the affinity for α1 and α2-adrenergic receptors than CH-1 . The studies carried out allow us to state that the highest affinity for α1-adrenergic receptors is demonstrated by compounds having a phenoxyethylpiperazine or phenylpiperazine group in their structure. The most advantageous for the antiarrythmic activity is the presence of the phenoxyethylpiperazine or phenylpiperazine group at the 7-position of theophylline, and the 2-morpholineethylamin}, abstract={o substituent at the 8-position. For hypotensive activity, however, the most advantageous is the presence of the phenoxyethylpiperazine group at the 7-position of theophylline, and the 2-benzylamino- or 2-pyridylmethylamino substituent at the 8-position. Hypotensive effect of the studied compounds most probably results from their α-adrenolytic and spasmolytic activity, whereas the antiarrythmic activity in the model of adrenaline arrythmia results from blocking α-adrenergic receptors.}, title={Affinity for adrenergic receptors and pharmacological activity of 7,8-disubstituted teophylline analogs}, type={Praca doktorska}, keywords={hypotensive activity, antiarrythmic activity, methyloxantines}, }