| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Frank S Menniti, Thomas A Chappie, Christopher J Schmid. PDE10A Inhibitors-Clinical Failure or Window Into Antipsychotic Drug Action? Frontiers in neuroscience. vol 14. 2021-02-10. PMID:33551724. |
with this in mind, we review the data on pde10a inhibition as a step toward back-translating the limited antipsychotic efficacy of pde10a inhibitors, hopefully to inform new efforts to develop better therapeutics to treat psychosis and schizophrenia. |
2021-02-10 |
2023-08-13 |
Not clear |
| Jonas Persson, K Szalisznyó, G Antoni, A Wall, D Fällmar, H Zora, R Bodé. Phosphodiesterase 10A levels are related to striatal function in schizophrenia: a combined positron emission tomography and functional magnetic resonance imaging study. European archives of psychiatry and clinical neuroscience. vol 270. issue 4. 2020-11-30. PMID:31119377. |
pharmacological inhibition of phosphodiesterase 10a (pde10a) is being investigated as a treatment option in schizophrenia. |
2020-11-30 |
2023-08-13 |
Not clear |
| Jonas Persson, K Szalisznyó, G Antoni, A Wall, D Fällmar, H Zora, R Bodé. Phosphodiesterase 10A levels are related to striatal function in schizophrenia: a combined positron emission tomography and functional magnetic resonance imaging study. European archives of psychiatry and clinical neuroscience. vol 270. issue 4. 2020-11-30. PMID:31119377. |
pde10a acts postsynaptically on striatal dopamine signaling by regulating neuronal excitability through its inhibition of cyclic adenosine monophosphate (camp), and we recently found it to be reduced in schizophrenia compared to controls. |
2020-11-30 |
2023-08-13 |
Not clear |
| Jonas Persson, K Szalisznyó, G Antoni, A Wall, D Fällmar, H Zora, R Bodé. Phosphodiesterase 10A levels are related to striatal function in schizophrenia: a combined positron emission tomography and functional magnetic resonance imaging study. European archives of psychiatry and clinical neuroscience. vol 270. issue 4. 2020-11-30. PMID:31119377. |
here, this finding of reduced pde10a in schizophrenia was followed up in the same sample to investigate the effect of reduced striatal pde10a on the neural and behavioral function of striatal and downstream basal ganglia regions. |
2020-11-30 |
2023-08-13 |
Not clear |
| Ahmed F Abdel-Magi. Potential of PDE10A Inhibitors as Treatment for Schizophrenia and Other Neurological Disorders. ACS medicinal chemistry letters. vol 9. issue 9. 2020-10-01. PMID:30258530. |
potential of pde10a inhibitors as treatment for schizophrenia and other neurological disorders. |
2020-10-01 |
2023-08-13 |
Not clear |
| Artur Świerczek, Agnieszka Jankowska, Grażyna Chłoń-Rzepa, Maciej Pawłowski, Elżbieta Wysk. Advances in the Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 2: Focus on Schizophrenia. Current drug targets. vol 20. issue 16. 2020-09-14. PMID:31368871. |
this review summarizes the results of recent preclinical and clinical studies on phosphodiesterase 10a (pde10a), which is highly expressed in the mammalian striatum, as a potential drug target for the treatment of schizophrenia. |
2020-09-14 |
2023-08-13 |
Not clear |
| Marie M Svedberg, Katarina Varnäs, Andrea Varrone, Nicholas Mitsios, Jan Mulder, Balázs Gulyás, Vahri Beaumont, Ignacio Munoz-Sanjuan, Margaret M Zaleska, Christopher J Schmidt, Christer Halldin, Ladislav Mrzlja. In vitro phosphodiesterase 10A (PDE10A) binding in whole hemisphere human brain using the PET radioligand [ Brain research. vol 1711. 2020-08-04. PMID:30664847. |
the phosphodiesterase 10a (pde10a) enzyme plays a central role in striatal signaling and is implicated in several neuropsychiatric disorders involving striatal pathology, such as huntingtońs disease (hd) and schizophrenia. |
2020-08-04 |
2023-08-13 |
human |
| David P Walling, Anindita Banerjee, Vikas Dawra, Stacey Boyer, Christopher J Schmidt, Nicholas DeMartini. Phosphodiesterase 10A Inhibitor Monotherapy Is Not an Effective Treatment of Acute Schizophrenia. Journal of clinical psychopharmacology. vol 39. issue 6. 2020-04-20. PMID:31688451. |
preclinical testing suggests that phosphodiesterase 10a (pde10a) inhibitors may provide a novel approach to treating psychosis associated with schizophrenia. |
2020-04-20 |
2023-08-13 |
Not clear |
| Misae Takakuwa, Yumi Watanabe, Kiichi Tanaka, Taketoshi Ishii, Kenta Kagaya, Hiroyuki Taniguchi, Jun Kotera, Kenji Hashimot. Antipsychotic-like effects of a novel phosphodiesterase 10A inhibitor T-251 in rodents. Pharmacology, biochemistry, and behavior. vol 185. 2020-02-26. PMID:31404565. |
pde10a is selectively expressed in medium spiny neurons in the striatum, suggesting the potential of pde10a inhibitors in the treatment of schizophrenia. |
2020-02-26 |
2023-08-13 |
human |
| Misae Takakuwa, Yumi Watanabe, Kiichi Tanaka, Taketoshi Ishii, Kenta Kagaya, Hiroyuki Taniguchi, Jun Kotera, Kenji Hashimot. Antipsychotic-like effects of a novel phosphodiesterase 10A inhibitor T-251 in rodents. Pharmacology, biochemistry, and behavior. vol 185. 2020-02-26. PMID:31404565. |
this study presents the pharmacological profile of a novel pde10a inhibitor, 2-[(e)-2-(7-fluoro-3-methylquinoxalin-2-yl)vinyl]-6-pyrrolidin-1-yl-n-(tetrahydro-2h-pyran-4-yl)pyrimidin-4-amine hydrochloride (t-251) in rodent models of schizophrenia. |
2020-02-26 |
2023-08-13 |
human |
| Agnieszka Jankowska, Artur Świerczek, Elżbieta Wyska, Alicja Gawalska, Adam Bucki, Maciej Pawłowski, Grażyna Chłoń-Rzep. Advances in Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 1: Overview of the Chemical and Biological Research. Current drug targets. vol 20. issue 1. 2020-02-24. PMID:30091414. |
the results of preclinical studies regarding the potential utility of pde10a inhibitors for the treatment of cns-related disorders, such as schizophrenia as well as huntington's and parkinson's diseases are also summarized. |
2020-02-24 |
2023-08-13 |
Not clear |
| Kazunori Suzuki, Haruhide Kimur. TAK-063, a novel PDE10A inhibitor with balanced activation of direct and indirect pathways, provides a unique opportunity for the treatment of schizophrenia. CNS neuroscience & therapeutics. vol 24. issue 7. 2019-06-10. PMID:29318783. |
tak-063, a novel pde10a inhibitor with balanced activation of direct and indirect pathways, provides a unique opportunity for the treatment of schizophrenia. |
2019-06-10 |
2023-08-13 |
Not clear |
| Paul Goldsmith, John Affinito, Maggie McCue, Max Tsai, Stefan Roepcke, Jinhui Xie, Lev Gertsik, Thomas A Mace. A Randomized Multiple Dose Pharmacokinetic Study of a Novel PDE10A Inhibitor TAK-063 in Subjects with Stable Schizophrenia and Japanese Subjects and Modeling of Exposure Relationships to Adverse Events. Drugs in R&D. vol 17. issue 4. 2018-06-29. PMID:29103081. |
a randomized multiple dose pharmacokinetic study of a novel pde10a inhibitor tak-063 in subjects with stable schizophrenia and japanese subjects and modeling of exposure relationships to adverse events. |
2018-06-29 |
2023-08-13 |
human |
| Paul Goldsmith, John Affinito, Maggie McCue, Max Tsai, Stefan Roepcke, Jinhui Xie, Lev Gertsik, Thomas A Mace. A Randomized Multiple Dose Pharmacokinetic Study of a Novel PDE10A Inhibitor TAK-063 in Subjects with Stable Schizophrenia and Japanese Subjects and Modeling of Exposure Relationships to Adverse Events. Drugs in R&D. vol 17. issue 4. 2018-06-29. PMID:29103081. |
tak-063 is a selective inhibitor of pde10a in clinical development for the treatment of schizophrenia. |
2018-06-29 |
2023-08-13 |
human |
| Yoichi Kadoh, Haruko Miyoshi, Takehiko Matsumura, Yoshihito Tanaka, Mitsuya Hongu, Mayumi Kimura, Kei Takedomi, Kenji Omori, Jun Kotera, Takashi Sasaki, Tamaki Kobayashi, Hiroyuki Taniguchi, Yumi Watanabe, Koki Kojima, Toshiaki Sakamoto, Toshiyuki Himiyama, Eiji Kawanish. Discovery of 2-[(E)-2-(7-Fluoro-3-methylquinoxalin-2-yl)vinyl]-6-pyrrolidin-1-yl-N-(tetrahydro-2H-pyran-4-yl)pyrimidin-4-amine Hydrochloride as a Highly Selective PDE10A Inhibitor. Chemical & pharmaceutical bulletin. vol 66. issue 3. 2018-03-27. PMID:29491258. |
therefore pde10a inhibitor is expected as a therapeutic method for psychosis disease such as schizophrenia. |
2018-03-27 |
2023-08-13 |
rat |
| Gunasingh J Masilamoni, Subramanian Uthayathas, Gerhard Koenig, Liza Leventhal, Stella M Pap. Effects of a novel phosphodiesterase 10A inhibitor in non-human primates: A therapeutic approach for schizophrenia with improved side effect profile. Neuropharmacology. vol 110. issue Pt A. 2018-02-22. PMID:27539962. |
phosphodiesterase 10a (pde10a) inhibitors have been considered as therapeutic agents for schizophrenia because the regulation of camp and cgmp in the striatum by pde10a plays an important role in the signaling mechanisms of the striatal-cortical network, and thereby in cognitive function. |
2018-02-22 |
2023-08-13 |
human |
| Gunasingh J Masilamoni, Subramanian Uthayathas, Gerhard Koenig, Liza Leventhal, Stella M Pap. Effects of a novel phosphodiesterase 10A inhibitor in non-human primates: A therapeutic approach for schizophrenia with improved side effect profile. Neuropharmacology. vol 110. issue Pt A. 2018-02-22. PMID:27539962. |
these findings suggest that frm-6308 has the adequate pharmacological profile to advance testing in clinical trials and demonstrate antipsychotic efficacy of pde10a inhibition for the treatment of schizophrenia patients. |
2018-02-22 |
2023-08-13 |
human |
| Akihiro Takano, Per Stenkrona, Vladimir Stepanov, Nahid Amini, Stefan Martinsson, Max Tsai, Paul Goldsmith, Jinhui Xie, Jingtao Wu, Tolga Uz, Christer Halldin, Thomas A Mace. A human [(11)C]T-773 PET study of PDE10A binding after oral administration of TAK-063, a PDE10A inhibitor. NeuroImage. vol 141. 2018-01-24. PMID:27423256. |
pde10a inhibitors are expected to be useful in treating neuropsychiatric disorders such as schizophrenia and huntington's disease. |
2018-01-24 |
2023-08-13 |
human |
| Jan-Philip Schülke, Nicholas J Brando. Current Understanding of PDE10A in the Modulation of Basal Ganglia Circuitry. Advances in neurobiology. vol 17. 2018-01-23. PMID:28956328. |
pde10a inhibition has been proposed as a novel way to modulate basal ganglia circuitry and to ameliorate symptoms in huntington's disease, parkinson's disease and schizophrenia. |
2018-01-23 |
2023-08-13 |
Not clear |
| Kazunori Suzuki, Akina Harada, Hirobumi Suzuki, Maki Miyamoto, Haruhide Kimur. TAK-063, a PDE10A Inhibitor with Balanced Activation of Direct and Indirect Pathways, Provides Potent Antipsychotic-Like Effects in Multiple Paradigms. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 41. issue 9. 2018-01-09. PMID:26849714. |
phosphodiesterase 10a (pde10a) inhibitors are expected to be novel drugs for schizophrenia through activation of both direct and indirect pathway medium spiny neurons. |
2018-01-09 |
2023-08-13 |
rat |