55176-88-0Relevant articles and documents
Synthesis and GABAA receptor activity of oxygen-bridged neurosteroid analogs
Alvarez, Lautaro D.,Veleiro, Adriana S.,Baggio, Ricardo F.,Garland, Maria T.,Edelsztein, Valeria C.,Coirini, Hector,Burton, Gerardo
, p. 3831 - 3838 (2008)
Three analogs of neuroactive steroids were prepared (4-6) in which 1,11- or 11,19-oxygen bridges give a constrained conformation. Their 3D structures were obtained by ab initio calculations and in the case of 3α-hydroxy-11,19-epoxypregn-4-ene-20-one (4), confirmed by X-ray analysis. Biological activity of the synthetic steroids was assayed in vitro using t-[3H]butylbicycloorthobenzoate as radiolabeled ligand for the GABAA receptor. The activity of compound 4 was similar to that of allopregnanolone (1). 1α,11α-Epoxypregnanolone (6) was more active than pregnanolone (2).
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Oliveto et al.
, p. 1505 (1953)
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Allopregnanolone and pregnanolone analogues modified in the C ring: Synthesis and activity
Slavíková, Barbora,Bujons, Jordi,Matyá?, Libor,Vidal, Miguel,Babot, Zoila,Kri?tofíková, Zdena,Su?ol, Cristina,Kasal, Alexander
, p. 2323 - 2336 (2013/06/04)
(25R)-3β-Hydroxy-5α-spirostan-12-one (hecogenin) and 11α-hydroxypregn-4-ene-3,20-dione (11α-hydroxyprogesterone) were used as starting materials for the synthesis of a series of 11- and 12-substituted derivatives of 5ξ-pregnanolone (3α-hydroxy-5α- pregnan-20-one and 3α-hydroxy-5β-pregnan-20-one), the principal neurosteroid acting via γ-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 [3H]flunitrazepam as radioligand in which allopregnanolone and its active analogues stimulated the binding to the GABAA 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.
NEW STEROID INHIBITORS OF PGP FOR USE FOR INHIBITING MULTIDRUG RESISTANCE
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Page/Page column 23, (2011/07/07)
The present invention relates to a compound of formula (I) for its use for reversing or inhibiting multidrug resistance.