MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively[1]. human PDE 10A|0.062 nM (IC50)|bovine PDE 10A|0.09 nM (IC50)
[1]. Koizumi Y, et al. Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety. Bioorg Med Chem. 2019 Jun 19.