Effect of synthetic steroids on GABAA receptor binding in rat brain

Autores
Rey, Mariana; Veleiro, Adriana Silvia; Ghini, Alberto Antonio; Kruse, Maria Sol; Burton, Gerardo; Coirini, Hector
Año de publicación
2015
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Neuroactive steroids (NAS), like allopregnanolone (A) and pregnanolone (P), bind to specifics sites on the GABAA receptor complex and modulate receptor function. They are capable to inhibit or stimulate the binding of GABAA receptor specific ligands, like t-butyl-bicyclophosphorothionate, flunitrazepam and muscimol. We have previously characterized a set of oxygen bridged synthetic steroids (SS) analogues to A or P using synaptosomes. Considering that the subunit composition of the GABAA receptor throughout the central nervous system affects the magnitude of the modulation of the GABAA receptor by NAS, here we evaluate the action of two selected SS, in brain sections containing cerebral cortex and hippocampus using quantitative receptor autoradiography. Both SS affected the binding of the three ligands in a similar way to A and P, with some differences on certain cerebral cortex layers according to the ligand used. One of the SS, the 3a-hydroxy-6,19-epoxypregn-4-ene-20-one (compound 5), behaved similarly to the natural NAS. However, significant differences with compound 5 were observed on hippocampus CA2 region, making it steroid suitable for a specific action. Those differences may be related to structural conformation of the SS and the subunits composition present on the receptor complex.
Fil: Rey, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina
Fil: Veleiro, Adriana Silvia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); Argentina
Fil: Ghini, Alberto Antonio. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); Argentina
Fil: Kruse, Maria Sol. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina
Fil: Burton, Gerardo. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); Argentina
Fil: Coirini, Hector. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina. Universidad de Buenos Aires. Facultad de Medicina; Argentina
Materia
Neurosteroids
Gabaa Receptor
Cerebral Cortex
Hippocampus
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/10573
Acceder
id CONICETDig_581757c10ab22759b317ce8e1214a506
oai_identifier_str oai:ri.conicet.gov.ar:11336/10573
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Effect of synthetic steroids on GABAA receptor binding in rat brainRey, MarianaVeleiro, Adriana SilviaGhini, Alberto AntonioKruse, Maria SolBurton, GerardoCoirini, HectorNeurosteroidsGabaa ReceptorCerebral CortexHippocampushttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Neuroactive steroids (NAS), like allopregnanolone (A) and pregnanolone (P), bind to specifics sites on the GABAA receptor complex and modulate receptor function. They are capable to inhibit or stimulate the binding of GABAA receptor specific ligands, like t-butyl-bicyclophosphorothionate, flunitrazepam and muscimol. We have previously characterized a set of oxygen bridged synthetic steroids (SS) analogues to A or P using synaptosomes. Considering that the subunit composition of the GABAA receptor throughout the central nervous system affects the magnitude of the modulation of the GABAA receptor by NAS, here we evaluate the action of two selected SS, in brain sections containing cerebral cortex and hippocampus using quantitative receptor autoradiography. Both SS affected the binding of the three ligands in a similar way to A and P, with some differences on certain cerebral cortex layers according to the ligand used. One of the SS, the 3a-hydroxy-6,19-epoxypregn-4-ene-20-one (compound 5), behaved similarly to the natural NAS. However, significant differences with compound 5 were observed on hippocampus CA2 region, making it steroid suitable for a specific action. Those differences may be related to structural conformation of the SS and the subunits composition present on the receptor complex.Fil: Rey, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); ArgentinaFil: Veleiro, Adriana Silvia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); ArgentinaFil: Ghini, Alberto Antonio. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); ArgentinaFil: Kruse, Maria Sol. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); ArgentinaFil: Burton, Gerardo. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); ArgentinaFil: Coirini, Hector. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina. Universidad de Buenos Aires. Facultad de Medicina; ArgentinaElsevier2015-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/10573Rey, Mariana; Veleiro, Adriana Silvia; Ghini, Alberto Antonio; Kruse, Maria Sol; Burton, Gerardo; et al.; Effect of synthetic steroids on GABAA receptor binding in rat brain; Elsevier; Neuroscience; 290; 2-2015; 138-1460306-45221873-7544enginfo:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0306452215000573info:eu-repo/semantics/altIdentifier/url/http://dx.doi.org/ 10.1016/j.neuroscience.2014.12.082info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:06:57Zoai:ri.conicet.gov.ar:11336/10573instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:06:57.626CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Effect of synthetic steroids on GABAA receptor binding in rat brain
title Effect of synthetic steroids on GABAA receptor binding in rat brain
spellingShingle Effect of synthetic steroids on GABAA receptor binding in rat brain
Rey, Mariana
Neurosteroids
Gabaa Receptor
Cerebral Cortex
Hippocampus
title_short Effect of synthetic steroids on GABAA receptor binding in rat brain
title_full Effect of synthetic steroids on GABAA receptor binding in rat brain
title_fullStr Effect of synthetic steroids on GABAA receptor binding in rat brain
title_full_unstemmed Effect of synthetic steroids on GABAA receptor binding in rat brain
title_sort Effect of synthetic steroids on GABAA receptor binding in rat brain
dc.creator.none.fl_str_mv Rey, Mariana
Veleiro, Adriana Silvia
Ghini, Alberto Antonio
Kruse, Maria Sol
Burton, Gerardo
Coirini, Hector
author Rey, Mariana
author_facet Rey, Mariana
Veleiro, Adriana Silvia
Ghini, Alberto Antonio
Kruse, Maria Sol
Burton, Gerardo
Coirini, Hector
author_role author
author2 Veleiro, Adriana Silvia
Ghini, Alberto Antonio
Kruse, Maria Sol
Burton, Gerardo
Coirini, Hector
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Neurosteroids
Gabaa Receptor
Cerebral Cortex
Hippocampus
topic Neurosteroids
Gabaa Receptor
Cerebral Cortex
Hippocampus
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Neuroactive steroids (NAS), like allopregnanolone (A) and pregnanolone (P), bind to specifics sites on the GABAA receptor complex and modulate receptor function. They are capable to inhibit or stimulate the binding of GABAA receptor specific ligands, like t-butyl-bicyclophosphorothionate, flunitrazepam and muscimol. We have previously characterized a set of oxygen bridged synthetic steroids (SS) analogues to A or P using synaptosomes. Considering that the subunit composition of the GABAA receptor throughout the central nervous system affects the magnitude of the modulation of the GABAA receptor by NAS, here we evaluate the action of two selected SS, in brain sections containing cerebral cortex and hippocampus using quantitative receptor autoradiography. Both SS affected the binding of the three ligands in a similar way to A and P, with some differences on certain cerebral cortex layers according to the ligand used. One of the SS, the 3a-hydroxy-6,19-epoxypregn-4-ene-20-one (compound 5), behaved similarly to the natural NAS. However, significant differences with compound 5 were observed on hippocampus CA2 region, making it steroid suitable for a specific action. Those differences may be related to structural conformation of the SS and the subunits composition present on the receptor complex.
Fil: Rey, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina
Fil: Veleiro, Adriana Silvia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); Argentina
Fil: Ghini, Alberto Antonio. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); Argentina
Fil: Kruse, Maria Sol. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina
Fil: Burton, Gerardo. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos Aplicados a la Química Orgánica (i); Argentina
Fil: Coirini, Hector. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina. Universidad de Buenos Aires. Facultad de Medicina; Argentina
description Neuroactive steroids (NAS), like allopregnanolone (A) and pregnanolone (P), bind to specifics sites on the GABAA receptor complex and modulate receptor function. They are capable to inhibit or stimulate the binding of GABAA receptor specific ligands, like t-butyl-bicyclophosphorothionate, flunitrazepam and muscimol. We have previously characterized a set of oxygen bridged synthetic steroids (SS) analogues to A or P using synaptosomes. Considering that the subunit composition of the GABAA receptor throughout the central nervous system affects the magnitude of the modulation of the GABAA receptor by NAS, here we evaluate the action of two selected SS, in brain sections containing cerebral cortex and hippocampus using quantitative receptor autoradiography. Both SS affected the binding of the three ligands in a similar way to A and P, with some differences on certain cerebral cortex layers according to the ligand used. One of the SS, the 3a-hydroxy-6,19-epoxypregn-4-ene-20-one (compound 5), behaved similarly to the natural NAS. However, significant differences with compound 5 were observed on hippocampus CA2 region, making it steroid suitable for a specific action. Those differences may be related to structural conformation of the SS and the subunits composition present on the receptor complex.
publishDate 2015
dc.date.none.fl_str_mv 2015-02
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/10573
Rey, Mariana; Veleiro, Adriana Silvia; Ghini, Alberto Antonio; Kruse, Maria Sol; Burton, Gerardo; et al.; Effect of synthetic steroids on GABAA receptor binding in rat brain; Elsevier; Neuroscience; 290; 2-2015; 138-146
0306-4522
1873-7544
url http://hdl.handle.net/11336/10573
identifier_str_mv Rey, Mariana; Veleiro, Adriana Silvia; Ghini, Alberto Antonio; Kruse, Maria Sol; Burton, Gerardo; et al.; Effect of synthetic steroids on GABAA receptor binding in rat brain; Elsevier; Neuroscience; 290; 2-2015; 138-146
0306-4522
1873-7544
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0306452215000573
info:eu-repo/semantics/altIdentifier/url/http://dx.doi.org/ 10.1016/j.neuroscience.2014.12.082
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1844613923795369984
score 13.070432

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