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| Description
| - The N-phenylpiperazine structures exhibit very extensive multiple receptor activities including the influencing of alfa1-adrenoceptors (alfa1-AR). Their antagonistic activity towards alfa1-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 alfa1-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 alfa1-AR subtypes holds promise for the discovery, projection and development of more specific selective drug molecules targeting only one alfa1-adrenoceptor subtype and making them free from side effects. Towards this aim wide-ranging modifications have been reported in the literature on the %22basic%22 structure of the N-phenylpiperazine-based molecules. The present paper deals with the affinity features of (substituted) N-phenylpiperazines towards alfa1-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.
- The N-phenylpiperazine structures exhibit very extensive multiple receptor activities including the influencing of alfa1-adrenoceptors (alfa1-AR). Their antagonistic activity towards alfa1-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 alfa1-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 alfa1-AR subtypes holds promise for the discovery, projection and development of more specific selective drug molecules targeting only one alfa1-adrenoceptor subtype and making them free from side effects. Towards this aim wide-ranging modifications have been reported in the literature on the %22basic%22 structure of the N-phenylpiperazine-based molecules. The present paper deals with the affinity features of (substituted) N-phenylpiperazines towards alfa1-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. (en)
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| Title
| - Relationship between chemical structure, binding affinity and selectivity towards alfa1-adrenoceptors in the group of substituted n-phenylpiperazines. Part 2*. compounds containing ethane-1,2-diyl connecting chain
- Relationship between chemical structure, binding affinity and selectivity towards alfa1-adrenoceptors in the group of substituted n-phenylpiperazines. Part 2*. compounds containing ethane-1,2-diyl connecting chain (en)
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| skos:prefLabel
| - Relationship between chemical structure, binding affinity and selectivity towards alfa1-adrenoceptors in the group of substituted n-phenylpiperazines. Part 2*. compounds containing ethane-1,2-diyl connecting chain
- Relationship between chemical structure, binding affinity and selectivity towards alfa1-adrenoceptors in the group of substituted n-phenylpiperazines. Part 2*. compounds containing ethane-1,2-diyl connecting chain (en)
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| skos:notation
| - RIV/62157124:16370/11:43870898!RIV12-MSM-16370___
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/62157124:16370/11:43870898
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - selectivity; affinity; alfa1-adrenoceptors; N-phenylpiperazines (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Acta Facultatis Pharmaceuticae Universitatis Comenianae Bratislava
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
| |
| http://linked.open...UplatneniVysledku
| |
| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Csöllei, Jozef
- Gališinová, Jana
- Malík, Ivan
- Sedlárová, Eva
- Adriamainty, Fils
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| issn
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| number of pages
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| http://bibframe.org/vocab/doi
| - 10.2478/v10219-011-0005-1
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| http://localhost/t...ganizacniJednotka
| |
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