TAK-063 | Selective PDE10A inhibitor

TAK-063 chemical structure

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TAK-063 (1238697-26-1) is a potent (IC50 = 0.3 nM), selective, and orally bioavailable inhibitor of phosphodiesterase 10A (PDE10A).1 It increased levels of cAMP and cGMP in mice and suppressed PCP-induced hyperlocomotion in mice. TAK-063 displayed antipsychotic-like activity in rats.2 It also displayed neuroprotective effects and ameliorated behavioral deficits in a mouse model of Huntington’s Disease.3 TAK-063 has displayed neuroprotective effects in mouse models of ischemic stroke.4,5

References/Citations:

  1. Kunitomo et al. (2014), Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazine-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor; J. Med. Chem. 57 9627
  2. Suzuki et al. (2015), In vivo pharmacological characterization of TAK-063, a potent and selective phosphodiesterase 10A inhibitor with antipsychotic-like activity in rats; J. Pharmacol. Exp. Ther. 352 471
  3. Harada et al. (2017), TAK-063, a Novel Phosphodiesterase 10A Inhibitor, Protects from Striatal Neurodegeneration and Ameliorates Behavioral Deficits in the R6/2 Mouse Model of Huntington’s Disease; J. Pharmacol. Exp. Ther. 360 75
  4. Beker et al. (2022), Phosphodiesterase 10A is a Critical Target for Neuroprotection in a Mouse Model of Ischemic Stroke; Mol. Neurobiol. 59 574
  5. Beker et al. (2022), Phosphodiesterase 10A deactivation induces long-term neurological recovery, Peri-infarct remodeling and pyramidal tract plasticity after transient focal cerebral ischemia in mice; Exp. Neurol. 358 114221
1238697-26-2, Balipodect, Balipodect supplier, PDE10A inhibitor, selective PDE10A inhibitor, TAK-063, TAK-063 supplier, TAK063
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Balipodect

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TAK-063 (1238697-26-1) is a potent (IC50 = 0.3 nM), selective, and orally bioavailable inhibitor of phosphodiesterase 10A (PDE10A).1 It increased levels of cAMP and cGMP in mice and suppressed PCP-induced hyperlocomotion in mice. TAK-063 displayed antipsychotic-like activity in rats.2 It also displayed neuroprotective effects and ameliorated behavioral deficits in a mouse model of Huntington’s Disease.3 TAK-063 has displayed neuroprotective effects in mouse models of ischemic stroke.4,5

References/Citations:

  1. Kunitomo et al. (2014), Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazine-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor; J. Med. Chem. 57 9627
  2. Suzuki et al. (2015), In vivo pharmacological characterization of TAK-063, a potent and selective phosphodiesterase 10A inhibitor with antipsychotic-like activity in rats; J. Pharmacol. Exp. Ther. 352 471
  3. Harada et al. (2017), TAK-063, a Novel Phosphodiesterase 10A Inhibitor, Protects from Striatal Neurodegeneration and Ameliorates Behavioral Deficits in the R6/2 Mouse Model of Huntington’s Disease; J. Pharmacol. Exp. Ther. 360 75
  4. Beker et al. (2022), Phosphodiesterase 10A is a Critical Target for Neuroprotection in a Mouse Model of Ischemic Stroke; Mol. Neurobiol. 59 574
  5. Beker et al. (2022), Phosphodiesterase 10A deactivation induces long-term neurological recovery, Peri-infarct remodeling and pyramidal tract plasticity after transient focal cerebral ischemia in mice; Exp. Neurol. 358 114221