Source:http://linkedlifedata.com/resource/pubmed/id/16722640
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
2006-5-25
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pubmed:abstractText |
A GABA(A) receptor study of several B-nor analogues of allopregnanolone and pregnanolone has been carried out. B-norallopregnanolone (i.e., 3alpha-hydroxy-7-nor-5alpha-pregnan-20-one) was found comparable to allopregnanolone when measured with labeled TBPS. Analogous results were obtained from their effect on neurons in culture: this time, both 3alpha-hydroxy-7-nor-5xi-pregnan-20-ones (5 and 6) were found to stimulate [3H]flunitrazepam binding and GABA-induced 36Cl- influx. These effects were inhibited by GABA(A) receptor antagonists. Other analogues carrying electronegative substituents (epoxides 9 and 10 and ketone 12) in the B ring were inactive. Similarly, B-normal ketones 17, and 18 and 6-azasteroids 20 and 21 were also inactive. B-Nor analogues 5 and 6 did not induce neurotoxicity at relevant concentrations. A computational analysis of active and inactive neurosteroid analogues allowed the proposal of a 3D pharmacophoric hypothesis of their interaction with the GABA(A) receptor.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anions,
http://linkedlifedata.com/resource/pubmed/chemical/Chlorides,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Modulators,
http://linkedlifedata.com/resource/pubmed/chemical/Pregnanolone,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3225-34
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16722640-Animals,
pubmed-meshheading:16722640-Anions,
pubmed-meshheading:16722640-Cell Survival,
pubmed-meshheading:16722640-Cells, Cultured,
pubmed-meshheading:16722640-Chlorides,
pubmed-meshheading:16722640-Computer Simulation,
pubmed-meshheading:16722640-GABA Modulators,
pubmed-meshheading:16722640-Male,
pubmed-meshheading:16722640-Models, Molecular,
pubmed-meshheading:16722640-Neocortex,
pubmed-meshheading:16722640-Neurons,
pubmed-meshheading:16722640-Pregnanolone,
pubmed-meshheading:16722640-Radioligand Assay,
pubmed-meshheading:16722640-Rats,
pubmed-meshheading:16722640-Rats, Wistar,
pubmed-meshheading:16722640-Receptors, GABA-A,
pubmed-meshheading:16722640-Structure-Activity Relationship
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pubmed:year |
2006
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pubmed:articleTitle |
Activity of B-nor analogues of neurosteroids on the GABA(A) receptor in primary neuronal cultures.
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pubmed:affiliation |
Institut d'Investigacions Biomèdiques de Barcelona, Consejo Superior de Investigaciones Científicas, CSIC-IDIBAPS, Barcelona, Spain.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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