| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Koen Van Laere, Rawaha U Ahmad, Hendra Hudyana, Sofie Celen, Kristof Dubois, Mark E Schmidt, Guy Bormans, Michel Kool. Human biodistribution and dosimetry of 18F-JNJ42259152, a radioligand for phosphodiesterase 10A imaging. European journal of nuclear medicine and molecular imaging. vol 40. issue 2. 2013-06-27. PMID:23160998. |
phosphodiesterase 10a (pde10a) is a camp/cgmp-hydrolysing enzyme with a central role in striatal signalling and implicated in neuropsychiatric disorders such as huntington's disease, parkinson's disease, schizophrenia and addiction. |
2013-06-27 |
2023-08-12 |
human |
| Jan Kehle. Phosphodiesterase 10A inhibitors: a 2009 - 2012 patent update. Expert opinion on therapeutic patents. vol 23. issue 1. 2013-06-04. PMID:23210904. |
the majority of companies have been focusing on the treatment of schizophrenia since preclinical evidence suggests that a pde10a inhibitor could provide antipsychotic, pro-cognitive and negative symptom efficacy. |
2013-06-04 |
2023-08-12 |
Not clear |
| Judith A Siuciak, Christine A Stric. Phosphodiesterase 10A inhibitors as a novel therapeutic approach for schizophrenia. Expert opinion on drug discovery. vol 2. issue 7. 2013-03-17. PMID:23484819. |
potent and selective pde10a inhibitors have recently been described in the scientific literature and their in vivo effects suggest the potential uses of pde10a inhibitors in cns disorders, particularly schizophrenia. |
2013-03-17 |
2023-08-12 |
Not clear |
| Sean M Smith, Jason M Uslaner, Christopher D Cox, Sarah L Huszar, Christopher E Cannon, Joshua D Vardigan, Donnie Eddins, Dawn M Toolan, Monika Kandebo, Lihang Yao, Izzat T Raheem, John D Schreier, Michael J Breslin, Paul J Coleman, John J Renge. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. vol 64. 2013-02-11. PMID:22750078. |
phosphodiesterase 10a (pde10a) is a novel target for the treatment of schizophrenia that may address multiple symptomatic domains associated with this disorder. |
2013-02-11 |
2023-08-12 |
rat |
| Sean M Smith, Jason M Uslaner, Christopher D Cox, Sarah L Huszar, Christopher E Cannon, Joshua D Vardigan, Donnie Eddins, Dawn M Toolan, Monika Kandebo, Lihang Yao, Izzat T Raheem, John D Schreier, Michael J Breslin, Paul J Coleman, John J Renge. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. vol 64. 2013-02-11. PMID:22750078. |
these findings suggest that pde10a inhibitors have the potential to impact multiple symptomatic domains of schizophrenia including positive symptoms and cognitive impairment. |
2013-02-11 |
2023-08-12 |
rat |
| Neil S Cutshall, Rene Onrust, Alex Rohde, Sasha Gragerov, Lauren Hamilton, Kevin Harbol, Hui-Rong Shen, Shawn McKee, Charles Zuta, Galina Gragerova, Vince Florio, Thomas N Wheeler, Jennifer L Gag. Novel 2-methoxyacylhydrazones as potent, selective PDE10A inhibitors with activity in animal models of schizophrenia. Bioorganic & medicinal chemistry letters. vol 22. issue 17. 2013-01-07. PMID:22841436. |
novel 2-methoxyacylhydrazones as potent, selective pde10a inhibitors with activity in animal models of schizophrenia. |
2013-01-07 |
2023-08-12 |
Not clear |
| Ginny D Ho, Shu-Wei Yang, Jennifer Smotryski, Ana Bercovici, Terry Nechuta, Elizabeth M Smith, William McElroy, Zheng Tan, Deen Tulshian, Brian McKittrick, William J Greenlee, Alan Hruza, Li Xiao, Diane Rindgen, Deborra Mullins, Mario Guzzi, Xiaoping Zhang, Carina Bleickardt, Robert Hodgso. The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia. Bioorganic & medicinal chemistry letters. vol 22. issue 2. 2012-08-24. PMID:22222034. |
the discovery of potent, selective, and orally active pyrazoloquinolines as pde10a inhibitors for the treatment of schizophrenia. |
2012-08-24 |
2023-08-12 |
rat |
| Yu-Tien Hsu, Guanghong Liao, Xiaoning Bi, Tetsushi Oka, Shigeki Tamura, Michel Baudr. The PDE10A inhibitor, papaverine, differentially activates ERK in male and female rat striatal slices. Neuropharmacology. vol 61. issue 8. 2012-08-01. PMID:21816164. |
the phosphodiesterase 10a (pde10a) is highly expressed within dopaminoreceptive medium spiny neurons (msns) of the striatum, which are implicated in various neurodegenerative diseases and psychiatric disorders, such as huntington's disease and schizophrenia. |
2012-08-01 |
2023-08-12 |
rat |
| Stefanie Dedeurwaerdere, Cindy Wintmolders, Greet Vanhoof, Xavier Langloi. Patterns of brain glucose metabolism induced by phosphodiesterase 10A inhibitors in the mouse: a potential translational biomarker. The Journal of pharmacology and experimental therapeutics. vol 339. issue 1. 2011-11-22. PMID:21742809. |
phosphodiesterase 10a (pde10a) inhibitors have recently been proposed as a new therapy for schizophrenia. |
2011-11-22 |
2023-08-12 |
mouse |
| Jan Kehler, Jacob Nielse. PDE10A inhibitors: novel therapeutic drugs for schizophrenia. Current pharmaceutical design. vol 17. issue 2. 2011-09-29. PMID:21355834. |
pde10a inhibitors: novel therapeutic drugs for schizophrenia. |
2011-09-29 |
2023-08-12 |
Not clear |
| Jan Kehler, Jacob Nielse. PDE10A inhibitors: novel therapeutic drugs for schizophrenia. Current pharmaceutical design. vol 17. issue 2. 2011-09-29. PMID:21355834. |
preclinical evidence in a range of animal models suggests that a pde10a inhibitor could provide efficacy on positive, cognitive and negative symptoms of schizophrenia and pde10a inhibitors are currently being evaluated in clinical trials for the treatment of schizophrenia. |
2011-09-29 |
2023-08-12 |
Not clear |
| Erik I Charych, Li-Xin Jiang, Frederick Lo, Kelly Sullivan, Nicholas J Brando. Interplay of palmitoylation and phosphorylation in the trafficking and localization of phosphodiesterase 10A: implications for the treatment of schizophrenia. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 30. issue 27. 2010-08-16. PMID:20610737. |
phosphodiesterase 10a (pde10a) is a striatum-enriched, dual-specific cyclic nucleotide phosphodiesterase that has gained considerable attention as a potential therapeutic target for psychiatric disorders such as schizophrenia. |
2010-08-16 |
2023-08-12 |
mouse |
| Patrick R Verhoest, Douglas S Chapin, Michael Corman, Kari Fonseca, John F Harms, Xinjun Hou, Eric S Marr, Frank S Menniti, Frederick Nelson, Rebecca O'Connor, Jayvardhan Pandit, Caroline Proulx-Lafrance, Anne W Schmidt, Christopher J Schmidt, Judith A Suiciak, Spiros Lira. 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. Journal of medicinal chemistry. vol 52. issue 16. 2010-07-01. PMID:19630403. |
this pde10a inhibitor is the first reported clinical entry for this mechanism in the treatment of schizophrenia. |
2010-07-01 |
2023-08-12 |
Not clear |
| Christine A Strick, Larry C James, Carol B Fox, Thomas F Seeger, Frank S Menniti, Christopher J Schmid. Alterations in gene regulation following inhibition of the striatum-enriched phosphodiesterase, PDE10A. Neuropharmacology. vol 58. issue 2. 2010-04-13. PMID:19765598. |
these findings support the hypothesis that pde10a modulates signal transduction in both striatal output pathways and suggest that pde10a inhibitors may offer a unique approach to the treatment of schizophrenia. |
2010-04-13 |
2023-08-12 |
mouse |
| Jan Kehler, John Paul Kilbur. Patented PDE10A inhibitors: novel compounds since 2007. Expert opinion on therapeutic patents. vol 19. issue 12. 2010-02-02. PMID:19939189. |
pde10a inhibition has generated much excitement as a potential novel mechanism for the treatment of the positive symptoms of schizophrenia. |
2010-02-02 |
2023-08-12 |
Not clear |
| Jan Kehler, John Paul Kilbur. Patented PDE10A inhibitors: novel compounds since 2007. Expert opinion on therapeutic patents. vol 19. issue 12. 2010-02-02. PMID:19939189. |
at least one pde10a inhibitor compound has been progressed to clinical phase ii for the treatment of schizophrenia. |
2010-02-02 |
2023-08-12 |
Not clear |
| Tom Chappie, John Humphrey, Frank Menniti, Chris Schmid. PDE10A inhibitors: an assessment of the current CNS drug discovery landscape. Current opinion in drug discovery & development. vol 12. issue 4. 2010-01-28. PMID:19562642. |
the inhibition of pde10a produces effects that modulate basal ganglia function in ways that suggest a particular therapeutic utility in the treatment of psychosis in schizophrenia. |
2010-01-28 |
2023-08-12 |
Not clear |
| Florence Sotty, Liliana P Montezinho, Björn Steiniger-Brach, Jacob Nielse. Phosphodiesterase 10A inhibition modulates the sensitivity of the mesolimbic dopaminergic system to D-amphetamine: involvement of the D1-regulated feedback control of midbrain dopamine neurons. Journal of neurochemistry. vol 109. issue 3. 2009-06-09. PMID:19236563. |
there is a growing body of evidence suggesting that targeting pde10a may be beneficial for the treatment of positive symptoms in schizophrenia. |
2009-06-09 |
2023-08-12 |
Not clear |
| C J Schmidt, D S Chapin, J Cianfrogna, M L Corman, M Hajos, J F Harms, W E Hoffman, L A Lebel, S A McCarthy, F R Nelson, C Proulx-LaFrance, M J Majchrzak, A D Ramirez, K Schmidt, P A Seymour, J A Siuciak, F D Tingley, R D Williams, P R Verhoest, F S Mennit. Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18287214. |
these new pharmacological tools enabled studies that provide further evidence that inhibition of pde10a represents an important new target for the treatment of schizophrenia and related disorders of basal ganglia function. |
2008-05-19 |
2023-08-12 |
Not clear |
| Frank S Menniti, Thomas A Chappie, John M Humphrey, Christopher J Schmid. Phosphodiesterase 10A inhibitors: a novel approach to the treatment of the symptoms of schizophrenia. Current opinion in investigational drugs (London, England : 2000). vol 8. issue 1. 2007-05-08. PMID:17263185. |
in addition, by enhancing corticostriatal signaling, pde10a inhibitors have the potential to improve some of the cognitive symptoms of schizophrenia. |
2007-05-08 |
2023-08-12 |
Not clear |