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Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
Cajina, Manuel; Nattini, Megan; Song, Dekun; Smagin, Gennady; Jørgensen, Erling B; Chandrasena, Gamini; Bundgaard, Christoffer; Toft, Dorthe Bach; Huang, Xinyan; Acher, Francine; Doller, Dario.
Afiliación
  • Cajina M; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
  • Nattini M; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
  • Song D; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
  • Smagin G; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
  • Jørgensen EB; H. Lundbeck A/S, Ottiliavej 9, 2500 Copenhagen-Valby, Denmark.
  • Chandrasena G; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
  • Bundgaard C; H. Lundbeck A/S, Ottiliavej 9, 2500 Copenhagen-Valby, Denmark.
  • Toft DB; H. Lundbeck A/S, Ottiliavej 9, 2500 Copenhagen-Valby, Denmark.
  • Huang X; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
  • Acher F; Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, UMR 8601 CNRS, Université Paris Descartes , 45 rue des Saints-Pères, 75270 Paris Cedex 06, France.
  • Doller D; Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, United States.
ACS Med Chem Lett ; 5(2): 119-23, 2014 Feb 13.
Article en En | MEDLINE | ID: mdl-24900783
LSP1-2111 is a group III metabotropic glutamate receptor agonist with preference toward the mGlu4 receptor subtype. This compound has been extensively used as a tool to explore the pharmacology of mGlu4 receptor activation in preclinical animal behavioral models. However, the blood-brain barrier penetration of this amino acid derivative has never been studied. We report studies on the central nervous system (CNS) disposition of LSP1-2111 using quantitative microdialysis in rat. Significant unbound concentrations of the drug relative to its in vitro binding affinity and functional potency were established in extracellular fluid (ECF). These findings support the use of LSP1-2111 to study the CNS pharmacology of mGlu4 receptor activation through orthosteric agonist mechanisms.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Tipo de estudio: Prognostic_studies Idioma: En Revista: ACS Med Chem Lett Año: 2014 Tipo del documento: Article País de afiliación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Tipo de estudio: Prognostic_studies Idioma: En Revista: ACS Med Chem Lett Año: 2014 Tipo del documento: Article País de afiliación: Estados Unidos