دورية أكاديمية
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
| العنوان: | Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist. |
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| المؤلفون: | 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. |
| المصدر: | ACS medicinal chemistry letters [ACS Med Chem Lett] 2013 Dec 12; Vol. 5 (2), pp. 119-23. Date of Electronic Publication: 2013 Dec 12 (Print Publication: 2014). |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE |
| أسماء مطبوعة: | Original Publication: Washington, D.C. : American Chemical Society |
| مستخلص: | 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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| فهرسة مساهمة: | Keywords: G protein-coupled receptors; Metabotropic glutamate receptors; mGlu4 receptor; orthosteric agonist |
| تواريخ الأحداث: | Date Created: 20140606 Date Completed: 20140605 Latest Revision: 20211021 |
| رمز التحديث: | 20221213 |
| مُعرف محوري في PubMed: | PMC4027608 |
| DOI: | 10.1021/ml400338f |
| PMID: | 24900783 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1948-5875 |
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| DOI: | 10.1021/ml400338f |