Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.

RATIONALE: MDPV (3,4-methylenedioxypyrovalerone) is a synthetic cathinone present in bath salts. It is a powerful psychostimulant and blocker of the dopamine transporter (DAT), like cocaine. It is known that acute exposure to psychostimulants induces rapid changes in DAT function. OBJECTIVES: To inv...

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Detalles Bibliográficos
Autores: López Arnau, Raúl, Duart Castells, Leticia, Aster, Barbara, Camarasa García, Jordi, Escubedo Rafa, Elena, Pubill Sánchez, David
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2018
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/162419
Acceso en línea:https://hdl.handle.net/2445/162419
Access Level:acceso abierto
Palabra clave:Farmacologia
Biosíntesi
Farmacocinètica
Cocaïna
Metabolisme
Drogues
Estimulants
Fisiologia
Rates
Dopamina
Pharmacology
Biosynthesis
Pharmacokinetics
Cocaine
Metabolism
Drugs of abuse
Stimulants
Physiology
Rats
Dopamine
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oai_identifier_str oai:recercat.cat:2445/162419
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repository_id_str
spelling Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.López Arnau, RaúlDuart Castells, LeticiaAster, BarbaraCamarasa García, JordiEscubedo Rafa, ElenaPubill Sánchez, DavidFarmacologiaBiosíntesiFarmacocinèticaCocaïnaMetabolismeDroguesEstimulantsFisiologiaRatesDopaminaPharmacologyBiosynthesisPharmacokineticsCocaineMetabolismDrugs of abuseStimulantsPhysiologyRatsDopamineRATIONALE: MDPV (3,4-methylenedioxypyrovalerone) is a synthetic cathinone present in bath salts. It is a powerful psychostimulant and blocker of the dopamine transporter (DAT), like cocaine. It is known that acute exposure to psychostimulants induces rapid changes in DAT function. OBJECTIVES: To investigate the effects of MDPV on DAT function comparing with cocaine. METHODS: Binding of [3H]WIN 35428 was performed on PC 12 cells treated with MDPV and washed. Rat striatal synaptosomes were incubated with MDPV or cocaine (1 μM) for 1 h and [3H]dopamine (DA) uptake was performed. Also, different treatments with MDPV or cocaine were performed in Sprague-Dawley rats to assess locomotor activity and ex vivo [3H]DA uptake. RESULTS: MDPV increased surface [3H]WIN 35428 binding on PC 12 cells. In vitro incubation of synaptosomes with MDPV produced significant increases in Vmax and KM for [3H]DA uptake. In synaptosomes from MDPV- (1.5 mg/kg, s.c.) and cocaine- (30 mg/kg, i.p.) treated rats, there was a significantly higher and more persistent increase in [3H]DA uptake in the case of MDPV than cocaine. Repeated doses of MDPV developed tolerance to this DAT upregulation and 24 h after the 5-day treatment with MDPV, [3H]DA uptake was reduced. However, a challenge with the same drugs after withdrawal recovered the DAT upregulation by both drugs and showed an increased response to MDPV vs the first dose. At the same time, animals were sensitized to the stereotypies induced by both psychostimulants. CONCLUSIONS: MDPV induces a rapid and reversible functional upregulation of DAT more powerfully and lasting than cocaine.Springer Verlag2020202020182020info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersion14 p.application/pdfhttps://hdl.handle.net/2445/162419Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésVersió postprint del document publicat a: https://doi.org/10.1007/s00213-018-5052-zPsychopharmacology, 2018, vol. 236, num. 3, p. 925-938https://doi.org/10.1007/s00213-018-5052-z(c) Springer Verlag, 2018info:eu-repo/semantics/openAccessoai:recercat.cat:2445/1624192026-05-29T05:05:01Z
dc.title.none.fl_str_mv Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
title Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
spellingShingle Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
López Arnau, Raúl
Farmacologia
Biosíntesi
Farmacocinètica
Cocaïna
Metabolisme
Drogues
Estimulants
Fisiologia
Rates
Dopamina
Pharmacology
Biosynthesis
Pharmacokinetics
Cocaine
Metabolism
Drugs of abuse
Stimulants
Physiology
Rats
Dopamine
title_short Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
title_full Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
title_fullStr Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
title_full_unstemmed Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
title_sort Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
dc.creator.none.fl_str_mv López Arnau, Raúl
Duart Castells, Leticia
Aster, Barbara
Camarasa García, Jordi
Escubedo Rafa, Elena
Pubill Sánchez, David
author López Arnau, Raúl
author_facet López Arnau, Raúl
Duart Castells, Leticia
Aster, Barbara
Camarasa García, Jordi
Escubedo Rafa, Elena
Pubill Sánchez, David
author_role author
author2 Duart Castells, Leticia
Aster, Barbara
Camarasa García, Jordi
Escubedo Rafa, Elena
Pubill Sánchez, David
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Farmacologia
Biosíntesi
Farmacocinètica
Cocaïna
Metabolisme
Drogues
Estimulants
Fisiologia
Rates
Dopamina
Pharmacology
Biosynthesis
Pharmacokinetics
Cocaine
Metabolism
Drugs of abuse
Stimulants
Physiology
Rats
Dopamine
topic Farmacologia
Biosíntesi
Farmacocinètica
Cocaïna
Metabolisme
Drogues
Estimulants
Fisiologia
Rates
Dopamina
Pharmacology
Biosynthesis
Pharmacokinetics
Cocaine
Metabolism
Drugs of abuse
Stimulants
Physiology
Rats
Dopamine
description RATIONALE: MDPV (3,4-methylenedioxypyrovalerone) is a synthetic cathinone present in bath salts. It is a powerful psychostimulant and blocker of the dopamine transporter (DAT), like cocaine. It is known that acute exposure to psychostimulants induces rapid changes in DAT function. OBJECTIVES: To investigate the effects of MDPV on DAT function comparing with cocaine. METHODS: Binding of [3H]WIN 35428 was performed on PC 12 cells treated with MDPV and washed. Rat striatal synaptosomes were incubated with MDPV or cocaine (1 μM) for 1 h and [3H]dopamine (DA) uptake was performed. Also, different treatments with MDPV or cocaine were performed in Sprague-Dawley rats to assess locomotor activity and ex vivo [3H]DA uptake. RESULTS: MDPV increased surface [3H]WIN 35428 binding on PC 12 cells. In vitro incubation of synaptosomes with MDPV produced significant increases in Vmax and KM for [3H]DA uptake. In synaptosomes from MDPV- (1.5 mg/kg, s.c.) and cocaine- (30 mg/kg, i.p.) treated rats, there was a significantly higher and more persistent increase in [3H]DA uptake in the case of MDPV than cocaine. Repeated doses of MDPV developed tolerance to this DAT upregulation and 24 h after the 5-day treatment with MDPV, [3H]DA uptake was reduced. However, a challenge with the same drugs after withdrawal recovered the DAT upregulation by both drugs and showed an increased response to MDPV vs the first dose. At the same time, animals were sensitized to the stereotypies induced by both psychostimulants. CONCLUSIONS: MDPV induces a rapid and reversible functional upregulation of DAT more powerfully and lasting than cocaine.
publishDate 2018
dc.date.none.fl_str_mv 2018
2020
2020
2020
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/162419
url https://hdl.handle.net/2445/162419
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: https://doi.org/10.1007/s00213-018-5052-z
Psychopharmacology, 2018, vol. 236, num. 3, p. 925-938
https://doi.org/10.1007/s00213-018-5052-z
dc.rights.none.fl_str_mv (c) Springer Verlag, 2018
info:eu-repo/semantics/openAccess
rights_invalid_str_mv (c) Springer Verlag, 2018
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 14 p.
application/pdf
dc.publisher.none.fl_str_mv Springer Verlag
publisher.none.fl_str_mv Springer Verlag
dc.source.none.fl_str_mv Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
reponame:Recercat. Dipósit de la Recerca de Catalunya
instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
instname_str Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
reponame_str Recercat. Dipósit de la Recerca de Catalunya
collection Recercat. Dipósit de la Recerca de Catalunya
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,811543

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