Positive allosteric modulator at mGlu4
= 290 nM in mGlu4
-expressing HEK 293 cells). Reverses haloperidol-induced catalepsy in rats; prevents attentional deficit and forelimb asymmetry in a rodent model of Parkinson's disease. Exhibits affinity for MAO-B and MAO-A (Ki
values are 0.72 μ
M and 8.5 μ
M respectively). Brain penetrant.
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The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Jones et al.