LSP4-2022 is a potent and brain-penetrant mGlu4 -selective orthosteric agonist, with an EC 50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity [1] [2].
References:
[1]. Goudet C, et al. A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential. FASEB J. 2012 Apr;26(4):1682-93.
[2]. Podkowa K, Rzeźniczek S, Marciniak M, Acher F, Pilc A, Pałucha-Poniewiera A. A novel mGlu4 selective agonist LSP4-2022 increases behavioral despair in mouse models of antidepressant action. Neuropharmacology. 2015 Oct;97:338-45.
References:
[1]. Goudet C, et al. A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential. FASEB J. 2012 Apr;26(4):1682-93.
[2]. Podkowa K, Rzeźniczek S, Marciniak M, Acher F, Pilc A, Pałucha-Poniewiera A. A novel mGlu4 selective agonist LSP4-2022 increases behavioral despair in mouse models of antidepressant action. Neuropharmacology. 2015 Oct;97:338-45.