GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol

Autores
Garcia, Daniel Asmed; Vendrell, Iolanda; Galofré, Mireia; Suñol, Cristina
Año de publicación
2008
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Thymol is a monoterpene that specifically interacts with synaptic neural functions in neuronal GABA-operated Cl- channels. Here we explore the effects of thymol, and propofol as positive control, on t-[35S]butylbicyclophosphorothionate ([35S]TBPS) binding in primary cultures of cortical neurons. The study includes a meaningful analysis of the effect of various exposure buffers, and their correlation with GABA released from cells, chloride influx through the GABAA receptor and GABA transporter activity. Cell viability was also determined. Thymol and propofol inhibited the binding of [35S]TBPS to cells exposed to Tris-citrate-NaCl buffer whereas a biphasic effect was observed in HEPES solution. The different effects of the two buffers analysed are due to the higher capacity of Tris-citrate-NaCl buffer to induce the release of endogenous GABA facilitating the binding of [35S]TBPS to its recognition site at the GABAA receptor. Released GABA in the presence of this buffer was inhibited by the neuronal GABA transporter inhibitor SKF 100330-A. Tris-citrate-NaCl buffer also induced a chloride influx, which was reverted by picrotoxinin. TBPS binding in living cells is facilitated by GABA released from the cells, which in turn activates basal GABAA receptor activity. The results deepen on the allosteric mechanism of thymol as positive modulator of the GABAA receptor. Furthermore, we corroborate [35S]TBPS binding as an important test to verify the capacity of drugs to act on and recognize a site at the GABAA receptor.
Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Departamento de Química. Cátedra de Química Biológica; Argentina. Consejo Superior de Investigaciones Científicas; España
Fil: Vendrell, Iolanda. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; España
Fil: Galofré, Mireia. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; España
Fil: Suñol, Cristina. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; España
Materia
[35s]Tbps Binding
Buffer Effect, Neuronal Gaba Transporter
Chloride Uptake
Gaba Release
Gabaa Receptor
Thymol
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/57583
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/57583
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymolGarcia, Daniel AsmedVendrell, IolandaGalofré, MireiaSuñol, Cristina[35s]Tbps BindingBuffer Effect, Neuronal Gaba TransporterChloride UptakeGaba ReleaseGabaa ReceptorThymolhttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Thymol is a monoterpene that specifically interacts with synaptic neural functions in neuronal GABA-operated Cl- channels. Here we explore the effects of thymol, and propofol as positive control, on t-[35S]butylbicyclophosphorothionate ([35S]TBPS) binding in primary cultures of cortical neurons. The study includes a meaningful analysis of the effect of various exposure buffers, and their correlation with GABA released from cells, chloride influx through the GABAA receptor and GABA transporter activity. Cell viability was also determined. Thymol and propofol inhibited the binding of [35S]TBPS to cells exposed to Tris-citrate-NaCl buffer whereas a biphasic effect was observed in HEPES solution. The different effects of the two buffers analysed are due to the higher capacity of Tris-citrate-NaCl buffer to induce the release of endogenous GABA facilitating the binding of [35S]TBPS to its recognition site at the GABAA receptor. Released GABA in the presence of this buffer was inhibited by the neuronal GABA transporter inhibitor SKF 100330-A. Tris-citrate-NaCl buffer also induced a chloride influx, which was reverted by picrotoxinin. TBPS binding in living cells is facilitated by GABA released from the cells, which in turn activates basal GABAA receptor activity. The results deepen on the allosteric mechanism of thymol as positive modulator of the GABAA receptor. Furthermore, we corroborate [35S]TBPS binding as an important test to verify the capacity of drugs to act on and recognize a site at the GABAA receptor.Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Departamento de Química. Cátedra de Química Biológica; Argentina. Consejo Superior de Investigaciones Científicas; EspañaFil: Vendrell, Iolanda. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; EspañaFil: Galofré, Mireia. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; EspañaFil: Suñol, Cristina. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; EspañaElsevier Science2008-12info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/57583Garcia, Daniel Asmed; Vendrell, Iolanda; Galofré, Mireia; Suñol, Cristina; GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol; Elsevier Science; European Journal of Pharmacology; 600; 1-3; 12-2008; 26-310014-2999CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0014299908010303info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejphar.2008.10.013info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:18:04Zoai:ri.conicet.gov.ar:11336/57583instacron: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 10:18:05.058CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
title GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
spellingShingle GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
Garcia, Daniel Asmed
[35s]Tbps Binding
Buffer Effect, Neuronal Gaba Transporter
Chloride Uptake
Gaba Release
Gabaa Receptor
Thymol
title_short GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
title_full GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
title_fullStr GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
title_full_unstemmed GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
title_sort GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol
dc.creator.none.fl_str_mv Garcia, Daniel Asmed
Vendrell, Iolanda
Galofré, Mireia
Suñol, Cristina
author Garcia, Daniel Asmed
author_facet Garcia, Daniel Asmed
Vendrell, Iolanda
Galofré, Mireia
Suñol, Cristina
author_role author
author2 Vendrell, Iolanda
Galofré, Mireia
Suñol, Cristina
author2_role author
author
author
dc.subject.none.fl_str_mv [35s]Tbps Binding
Buffer Effect, Neuronal Gaba Transporter
Chloride Uptake
Gaba Release
Gabaa Receptor
Thymol
topic [35s]Tbps Binding
Buffer Effect, Neuronal Gaba Transporter
Chloride Uptake
Gaba Release
Gabaa Receptor
Thymol
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Thymol is a monoterpene that specifically interacts with synaptic neural functions in neuronal GABA-operated Cl- channels. Here we explore the effects of thymol, and propofol as positive control, on t-[35S]butylbicyclophosphorothionate ([35S]TBPS) binding in primary cultures of cortical neurons. The study includes a meaningful analysis of the effect of various exposure buffers, and their correlation with GABA released from cells, chloride influx through the GABAA receptor and GABA transporter activity. Cell viability was also determined. Thymol and propofol inhibited the binding of [35S]TBPS to cells exposed to Tris-citrate-NaCl buffer whereas a biphasic effect was observed in HEPES solution. The different effects of the two buffers analysed are due to the higher capacity of Tris-citrate-NaCl buffer to induce the release of endogenous GABA facilitating the binding of [35S]TBPS to its recognition site at the GABAA receptor. Released GABA in the presence of this buffer was inhibited by the neuronal GABA transporter inhibitor SKF 100330-A. Tris-citrate-NaCl buffer also induced a chloride influx, which was reverted by picrotoxinin. TBPS binding in living cells is facilitated by GABA released from the cells, which in turn activates basal GABAA receptor activity. The results deepen on the allosteric mechanism of thymol as positive modulator of the GABAA receptor. Furthermore, we corroborate [35S]TBPS binding as an important test to verify the capacity of drugs to act on and recognize a site at the GABAA receptor.
Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Departamento de Química. Cátedra de Química Biológica; Argentina. Consejo Superior de Investigaciones Científicas; España
Fil: Vendrell, Iolanda. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; España
Fil: Galofré, Mireia. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; España
Fil: Suñol, Cristina. Consejo Superior de Investigaciones Científicas; España. Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública; España
description Thymol is a monoterpene that specifically interacts with synaptic neural functions in neuronal GABA-operated Cl- channels. Here we explore the effects of thymol, and propofol as positive control, on t-[35S]butylbicyclophosphorothionate ([35S]TBPS) binding in primary cultures of cortical neurons. The study includes a meaningful analysis of the effect of various exposure buffers, and their correlation with GABA released from cells, chloride influx through the GABAA receptor and GABA transporter activity. Cell viability was also determined. Thymol and propofol inhibited the binding of [35S]TBPS to cells exposed to Tris-citrate-NaCl buffer whereas a biphasic effect was observed in HEPES solution. The different effects of the two buffers analysed are due to the higher capacity of Tris-citrate-NaCl buffer to induce the release of endogenous GABA facilitating the binding of [35S]TBPS to its recognition site at the GABAA receptor. Released GABA in the presence of this buffer was inhibited by the neuronal GABA transporter inhibitor SKF 100330-A. Tris-citrate-NaCl buffer also induced a chloride influx, which was reverted by picrotoxinin. TBPS binding in living cells is facilitated by GABA released from the cells, which in turn activates basal GABAA receptor activity. The results deepen on the allosteric mechanism of thymol as positive modulator of the GABAA receptor. Furthermore, we corroborate [35S]TBPS binding as an important test to verify the capacity of drugs to act on and recognize a site at the GABAA receptor.
publishDate 2008
dc.date.none.fl_str_mv 2008-12
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/11336/57583
Garcia, Daniel Asmed; Vendrell, Iolanda; Galofré, Mireia; Suñol, Cristina; GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol; Elsevier Science; European Journal of Pharmacology; 600; 1-3; 12-2008; 26-31
0014-2999
CONICET Digital
CONICET
url http://hdl.handle.net/11336/57583
identifier_str_mv Garcia, Daniel Asmed; Vendrell, Iolanda; Galofré, Mireia; Suñol, Cristina; GABA released from cultured cortical neurons influences the modulation of t-[35S]butylbicyclophosphorothionate binding at the GABAA receptor: Effects of thymol; Elsevier Science; European Journal of Pharmacology; 600; 1-3; 12-2008; 26-31
0014-2999
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0014299908010303
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejphar.2008.10.013
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier Science
publisher.none.fl_str_mv Elsevier Science
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
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score 13.070432

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