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rdf:type
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Description
| - (25R)-3 beta-Hydroxy-5 alpha-spirostan-12-one (hecogenin) and 11 alpha-hydroxypregn-4-ene-3,20-dione (11 alpha-hydroxyprogesterone) were used as starting materials for the synthesis of a series of 11- and 12-substituted derivatives of 5 xi-pregnanolone (3 alpha-hydroxy-5 alpha-pregnan-20-one and 3 alpha-hydroxy-5 beta-pregnan-20-one), the principal neurosteroid acting via gamma-aminobutyric acid (GABA). These analogues were designed to study the structural requirements of the corresponding GABA(A) receptor. Their biological activity was measured by in vitro test with [H-3]flunitrazepam as radio-ligand in which allopregnanolone and its active analogues stimulated the binding to the GABA(A) receptor. Analysis of the SAR data suggests dependence of the flunitrazepam binding activity on the hydrophobic-hydrophilic balance of the groups at the C-ring edge rather than on specific interactions between them and the receptor.
- (25R)-3 beta-Hydroxy-5 alpha-spirostan-12-one (hecogenin) and 11 alpha-hydroxypregn-4-ene-3,20-dione (11 alpha-hydroxyprogesterone) were used as starting materials for the synthesis of a series of 11- and 12-substituted derivatives of 5 xi-pregnanolone (3 alpha-hydroxy-5 alpha-pregnan-20-one and 3 alpha-hydroxy-5 beta-pregnan-20-one), the principal neurosteroid acting via gamma-aminobutyric acid (GABA). These analogues were designed to study the structural requirements of the corresponding GABA(A) receptor. Their biological activity was measured by in vitro test with [H-3]flunitrazepam as radio-ligand in which allopregnanolone and its active analogues stimulated the binding to the GABA(A) receptor. Analysis of the SAR data suggests dependence of the flunitrazepam binding activity on the hydrophobic-hydrophilic balance of the groups at the C-ring edge rather than on specific interactions between them and the receptor. (en)
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Title
| - Allopregnanolone and pregnanolone analogues modified in the C ring: synthesis and activity
- Allopregnanolone and pregnanolone analogues modified in the C ring: synthesis and activity (en)
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skos:prefLabel
| - Allopregnanolone and pregnanolone analogues modified in the C ring: synthesis and activity
- Allopregnanolone and pregnanolone analogues modified in the C ring: synthesis and activity (en)
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skos:notation
| - RIV/00023752:_____/13:43914448!RIV14-MZ0-00023752
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http://linked.open...avai/predkladatel
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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/00023752:_____/13:43914448
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - modulation; a receptors; analysis comsia; anesthetic steroids; neuroactive steroids; neurosteroid analogs; gaba(a) receptors; primary neuronal cultures; H-3 flunitrazepam binding; famma-aminobutyric-ACID (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Journal of Medicinal Chemistry
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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
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Kasal, Alexander
- Slavíková, Barbora
- Krištofiková, Zdena
- Babot, Zoila
- Bujons, Jordi
- Matyáš, Libor
- Sunol, Cristina
- Vidal, Miguel
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http://linked.open...ain/vavai/riv/wos
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issn
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number of pages
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http://bibframe.org/vocab/doi
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