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dc.contributor.author
Seeman, Philip
dc.contributor.author
Caruso, Carla Mariana
dc.contributor.author
Lasaga, Mercedes Isabel
dc.date.available
2020-06-29T14:31:03Z
dc.date.issued
2008-02
dc.identifier.citation
Seeman, Philip; Caruso, Carla Mariana; Lasaga, Mercedes Isabel; Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268; Veterinary and Human Toxicology; Synapse; 62; 2; 2-2008; 154-158
dc.identifier.issn
0887-4476
dc.identifier.uri
http://hdl.handle.net/11336/108389
dc.description.abstract
Because glutamate compounds alter the release of dopamine and prolactin, the present study examined whether group II metabotropic receptor agonists, LY 354,740 and LY 379,268, had any direct in vitro action on dopamine D2 receptors on rat striatal tissue, cloned D2Long receptors, and prolactin release from anterior pituitary cells. In competition versus the D2-specific ligand [(3)H]domperidone, LY 354,740 had a dissociation constant of 24 nM at D2(High) (the functional high-affinity state of dopamine D2 receptors), while the value for LY 379,268 was 21 nM. LY 354,740 also stimulated by 50% the incorporation of [(35)S]-GTP-gamma-S at a concentration of 120 nM, but its maximal stimulation was only 22% of the maximum elicited by dopamine. LY 379,268 stimulated by 50% the incorporation of [(35)S]-GTP-gamma-S at 280 nM, but its maximal stimulation was also only 22% of the maximum elicited by dopamine. However, both LY 354,740 and LY 379,268 potently inhibited the dopamine-induced incorporation of [(35)S]-GTP-gamma-S with inhibitory Ki values of 43 nM and 30 nM, respectively. The release of prolactin from rat isolated anterior pituitary cells in culture was 50% inhibited by 20 nM LY 379,268 and by 100 nM LY 354,740. These Ki values are similar to those known for the mGluR II receptor, suggesting that these compounds may have both glutamate and dopamine actions in vivo. The dopamine agonist and antagonist actions of these compounds indicate that these drugs have properties of a dopamine partial agonist, and may, therefore, have antipsychotic action.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Veterinary and Human Toxicology
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
D2 RECEPTORS
dc.subject
GROUP II METABOTROPIC RECEPTORS
dc.subject
PROLACTIN
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Fisiología
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Medicina Básica
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CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-05-11T15:48:55Z
dc.journal.volume
62
dc.journal.number
2
dc.journal.pagination
154-158
dc.journal.pais
Estados Unidos
dc.journal.ciudad
New York
dc.description.fil
Fil: Seeman, Philip. University of Toronto; Canadá
dc.description.fil
Fil: Caruso, Carla Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Biomédicas. Universidad de Buenos Aires. Facultad de Medicina. Instituto de Investigaciones Biomédicas; Argentina
dc.description.fil
Fil: Lasaga, Mercedes Isabel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Biomédicas. Universidad de Buenos Aires. Facultad de Medicina. Instituto de Investigaciones Biomédicas; Argentina
dc.journal.title
Synapse
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1002/syn.20482
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://pubmed.ncbi.nlm.nih.gov/18000815/
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