Mesdopetam (IRL790) is a novel dopamine transmission modulator and dopamine D3 receptor antagonist with Ki/IC50 of 0.09/0.41 uM.
IRL790 also shows sub-micromolar affinities at DA D2 and σ1 receptors, and micromolar affinities at 5-HT1a, 5-HT2a, and 5-HT7 receptors, does not show any agonist-like properties at D2, D3, 5-HT2, or 5-HT7 receptors.
IRL790 displays balancing effects on aberrant motor phenotypes, reducing l-DOPA-induced dyskinesias in the rodent 6-hydroxydopamine lesion model and reducing psychostimulant-induced locomotor hyperactivity elicited by pretreatment with either d-amphetamine or dizocilpine, without negatively impacting normal motor performance.
IRL790 is active in models of perturbed dopaminergic and glutamatergic signaling, including rodent 6-hydroxydopamine l-DOPA-induced dyskinesias and psychostimulant-induced hyperactivity, in a dose range that does not impair normal behavior.