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dc.contributor.author Suñol, Cristina
dc.contributor.author Garcia, Daniel Asmed
dc.contributor.author Bujons, Jordi
dc.contributor.author Kristofikova, Zdena
dc.contributor.author Matyas, Libor
dc.contributor.author Babot, Zoila
dc.contributor.author Kasal, Alexander
dc.date.available 2018-08-14T20:01:02Z
dc.date.issued 2006-06
dc.identifier.citation Suñol, Cristina; Garcia, Daniel Asmed; Bujons, Jordi; Kristofikova, Zdena; Matyas, Libor; et al.; Activity of B-nor analogues of neurosteroids on the GABAA receptor in primary neuronal cultures; American Chemical Society; Journal of Medicinal Chemistry; 49; 11; 6-2006; 3225-3234
dc.identifier.issn 0022-2623
dc.identifier.uri http://hdl.handle.net/11336/55491
dc.description.abstract A GABAA receptor study of several B-nor analogues of allopregnanolone and pregnanolone has been carried out. B-Norallopregnanolone (i.e., 3α-hydroxy-7-nor-5α-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 3α-hydroxy-7-nor-5ξ-pregnan-20-ones (5 and 6) were found to stimulate [3H]flunitrazepam binding and GABA-induced 36Cl - influx. These effects were inhibited by GABAA 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 GABAA receptor. © 2006 American Chemical Society.
dc.format application/pdf
dc.language.iso eng
dc.publisher American Chemical Society
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject Neurosteroids
dc.subject GABAA receptor
dc.subject Pharmacophore model
dc.subject Receptor binding and chloride flux
dc.subject.classification Otras Ciencias Biológicas
dc.subject.classification Ciencias Biológicas
dc.subject.classification CIENCIAS NATURALES Y EXACTAS
dc.title Activity of B-nor analogues of neurosteroids on the GABAA receptor in primary neuronal cultures
dc.type info:eu-repo/semantics/article
dc.type info:ar-repo/semantics/artículo
dc.type info:eu-repo/semantics/publishedVersion
dc.date.updated 2018-08-13T17:05:36Z
dc.journal.volume 49
dc.journal.number 11
dc.journal.pagination 3225-3234
dc.journal.pais Estados Unidos
dc.journal.ciudad Washington
dc.description.fil Fil: Suñol, Cristina. Consejo Superior de Investigaciones Científicas; España
dc.description.fil Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Consejo Superior de Investigaciones Científicas; España
dc.description.fil Fil: Bujons, Jordi. Consejo Superior de Investigaciones Científicas; España
dc.description.fil Fil: Kristofikova, Zdena. Academy of Sciences of the Czech Republic; República Checa
dc.description.fil Fil: Matyas, Libor. Academy of Sciences of the Czech Republic; República Checa
dc.description.fil Fil: Babot, Zoila. Consejo Superior de Investigaciones Científicas; España
dc.description.fil Fil: Kasal, Alexander. Academy of Sciences of the Czech Republic; República Checa
dc.journal.title Journal of Medicinal Chemistry
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/doi/https://dx.doi.org/10.1021/jm060002f
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/abs/10.1021/jm060002f
dc.conicet.fuente individual


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