Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
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ABSTRACT:
SUBMITTER: Cajina M
PROVIDER: S-EPMC4027608 | biostudies-literature | 2014 Feb
REPOSITORIES: biostudies-literature
Publications
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
Cajina Manuel M Nattini Megan M Song Dekun D Smagin Gennady G Jørgensen Erling B EB Chandrasena Gamini G Bundgaard Christoffer C Toft Dorthe Bach DB Huang Xinyan X Acher Francine F Doller Dario D
ACS medicinal chemistry letters 20131212 2
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 unbou ...[more]
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