%0 Journal Article
%T Relationship between chemical structure, binding affinity and selectivity towards ¦Á1-adrenoceptors in the group of substituted n-phenylpiperazines. Part 2*. compounds containing ethane-1,2-diyl connecting chain
%A I. Mal¨ªk
%A E. Sedl¨¢rov¨¢
%A F. Andriamainty
%A J. Gali inov¨¢
%A J. Cs llei
%J Acta Facultatis Pharmaceuticae Universitatis Comenianae
%D 2011
%I 
%R 10.2478/v10219-011-0005-1
%X The N-phenylpiperazine structures exhibit very extensive multiple receptor activities including the influencing of ¦Á1-adrenoceptors (¦Á1-AR). Their antagonistic activity towards ¦Á1-AR is intensively applied in the therapy of cardiovascular system diseases - e. g. hypertension as well as in the treatment of benign prostatic hyperplasia. The limited ratio of selective effect on the specific subtypes of the ¦Á1-AR by certain drugs used in the practice (azosine-type structures) leads to multiple side effects which includes postural hypotension, syncope or first dose phenomena. The existence of multiple ¦Á1-AR subtypes holds promise for the discovery, projection and development of more specific selective drug molecules targeting only one ¦Á1-adrenoceptor subtype and making them free from side effects. Towards this aim wide-ranging modifications have been reported in the literature on the "basic" structure of the N-phenylpiperazine-based molecules. The present paper deals with the affinity features of (substituted) N-phenylpiperazines towards ¦Á1-ARs in which the structure is a connecting chain formed by (unsubstituted) ethane-1,2-diyl moiety bonded through certain atom or group (S, O, NH, NHCO-fragment, respectively) at the lipophilic part of the molecule.
%K N-phenylpiperazines
%K ¦Á 1-adrenoceptors
%K affinity
%K selectivity
%U http://versita.metapress.com/content/l465316n7362w6l0/?p=12ead558b14f4d18ba07dea5c2cef045&pi=4