1 research outputs found
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist
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 <i>in vitro</i> 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