PF-2545920 | PDE10A inhibitor

PF-2545920 chemical structure

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PF-2545920 (898562-94-2) is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A), IC50 =  0.37 nM.1 Active in a number of animal models for antipsychotic activity.2 Suppresses microglial activation in LPA-induced neuroinflammation and MPTP-induced Parkinson’s disease models.3 Suppresses proliferation of human glioblastoma cells.4 Novel agent for stimulation of sperm motility.5 Brain penetrant.

References/Citations:

  1. Verhoest et al. (2009), Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia; J. Med. Chem., 52 5188
  2. Grauer et al. (2009), Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia; J. Pharmacol. Exp. Ther., 331 574
  3. Kim et al. (2021), The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson’s Disease Mouse Models; J. Neuroimmune Pharmacol., 16 470
  4. Kopanitsa et al. (2021), Suppression of Proliferation of Human Glioblastoma Cells by Combined Phosphodiesterase and Multidrug Resistance-Associated Protein 1 Inhibition; Int. J. Mol. Sci., 22 9965
  5. Yang et al. (2023), Phosphodiesterase 10A inhibitor PF-2545920 as a prospective agent for the clinical promotion of sperm motility; J. Androl., 25 608
898562-94-2, mardepodect, Mardepodect supplier, MP-10, PDE10A inhibitor, PF-2545920, PF-2545920 supplier, PF-920, PF2545920
Alternate Name:
Mardepodect; PF-920; MP-10

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PF-2545920 (898562-94-2) is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A), IC50 =  0.37 nM.1 Active in a number of animal models for antipsychotic activity.2 Suppresses microglial activation in LPA-induced neuroinflammation and MPTP-induced Parkinson’s disease models.3 Suppresses proliferation of human glioblastoma cells.4 Novel agent for stimulation of sperm motility.5 Brain penetrant.

References/Citations:

  1. Verhoest et al. (2009), Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia; J. Med. Chem., 52 5188
  2. Grauer et al. (2009), Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia; J. Pharmacol. Exp. Ther., 331 574
  3. Kim et al. (2021), The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson’s Disease Mouse Models; J. Neuroimmune Pharmacol., 16 470
  4. Kopanitsa et al. (2021), Suppression of Proliferation of Human Glioblastoma Cells by Combined Phosphodiesterase and Multidrug Resistance-Associated Protein 1 Inhibition; Int. J. Mol. Sci., 22 9965
  5. Yang et al. (2023), Phosphodiesterase 10A inhibitor PF-2545920 as a prospective agent for the clinical promotion of sperm motility; J. Androl., 25 608