Results 1 to 10 of about 4,588 (202)

A Novel PDE10A Inhibitor for Tourette Syndrome and Other Movement Disorders [PDF]

Cells
Background: Tourette syndrome is a neurodevelopmental movement disorder involving basal ganglia dysfunction. PDE10A inhibitors modulate signaling in the striatal basal ganglia nuclei and are thus of interest as potential therapeutics in treating Tourette
Randall D. Marshall, Frank S. Menniti, Mark A. Tepper   +2 more
doaj   +4 more sources

Phosphodiesterase 10A (PDE10A): Regulator of Dopamine Agonist-Induced Gene Expression in the Striatum [PDF]

Cells, 2022
Dopamine and other neurotransmitters have the potential to induce neuroplasticity in the striatum via gene regulation. Dopamine receptor-mediated gene regulation relies on second messenger cascades that involve cyclic nucleotides to relay signaling from ...
Ryan Bonate, Gabriela Kurek, Michael Hrabak, Santanna Patterson, Fernando Padovan-Neto, Anthony R. West, Heinz Steiner   +6 more
doaj   +3 more sources

PDE10A Inhibitors—Clinical Failure or Window Into Antipsychotic Drug Action? [PDF]

Frontiers in Neuroscience, 2021
PDE10A, a phosphodiesterase that inactivates both cAMP and cGMP, is a unique signaling molecule in being highly and nearly exclusively expressed in striatal medium spiny neurons.
Frank S. Menniti, Thomas A. Chappie, Christopher J. Schmidt   +2 more
doaj   +3 more sources

PDE10A Inhibition Reduces NLRP3 Activation and Pyroptosis in Sepsis and Nerve Injury. [PDF]

Int J Mol Sci
Cell death and inflammation are key innate immune responses, but excessive activation can cause tissue damage. The NLRP3 inflammasome is a promising target for reducing inflammation and promoting recovery.
Berk BC, Chávez CL, George Hsu C.
europepmc   +4 more sources

Evaluation of the acute oral toxicity and antipsychotic activity of a dual inhibitor of PDE1B and PDE10A in rat model of schizophrenia

PLoS ONE, 2022
Phosphodiesterase 1B (PDE1B) and PDE10A are dual-specificity PDEs that hydrolyse both cyclic adenosine monophosphate and cyclic guanosine monophosphate, and are highly expressed in the striatum.
Mayasah Al-Nema, Anand Gaurav, Ming Tatt Lee, Patrick Okechukwu, Piyarat Nimmanpipug, Vannajan Sanghiran Lee   +5 more
doaj   +5 more sources

Magnetic resonance imaging detects white adipose tissue beiging in mice following PDE10A inhibitor treatment [PDF]

Journal of Lipid Research, 2023
Weight gain is a common harmful side effect of atypical antipsychotics used for schizophrenia treatment. Conversely, treatment with the novel phosphodiesterase-10A (PDE10A) inhibitor MK-8189 in clinical trials led to significant weight reduction ...
Michal R. Tomaszewski, Xiangjun Meng, Hyking D. Haley, Charles M. Harrell, Terrence P. Mcdonald, Corin O. Miller, Sean M. Smith   +6 more
doaj   +3 more sources

In Silico study of PDE10A inhibitors for schizophrenia: molecular docking, ADMET and DFT analysis

Discover Chemistry
Recently, interest in phosphodiesterase 10 A inhibitors has increased for schizophrenia treatment. Medicinal chemists have extensively worked on developing potent PDE10A inhibitors with minimal side effects.
Ashutosh Kharwar, Akanksha Verma, Anjani Kumar Tiwari   +2 more
doaj   +3 more sources

Inhibition of CXCR2 enhances CNS remyelination via modulating PDE10A/cAMP signaling pathway

Neurobiology of Disease, 2023
CXC chemokine receptor 2 (CXCR2) plays an important role in demyelinating diseases, but the detailed mechanisms were not yet clarified. In the present study, we mainly investigated the critical function and the potential molecular mechanisms of CXCR2 on ...
Cheng Ju, Fangyu Yuan, Lu Wang, Caixia Zang, Jingwen Ning, Meiyu Shang, Jingwei Ma, Gen Li, Yang Yang, Qiuzhu Chen, Yueqi Jiang, Fangfang Li, Xiuqi Bao, Dan Zhang   +13 more
doaj   +2 more sources

Phosphodiesterase 10A (PDE10A) as a novel target to suppress β-catenin and RAS signaling in epithelial ovarian cancer

Journal of Ovarian Research, 2022
A leading theory for ovarian carcinogenesis proposes that inflammation associated with incessant ovulation is a driver of oncogenesis. Consistent with this theory, nonsteroidal anti-inflammatory drugs (NSAIDs) exert promising chemopreventive activity for
Rebecca M. Borneman, Elaine Gavin, Alla Musiyenko, Wito Richter, Kevin J. Lee, David K. Crossman, Joel F. Andrews, Annelise M. Wilhite, Steven McClellan, Ileana Aragon, Antonio B. Ward, Xi Chen, Adam B. Keeton, Kristy Berry, Gary A. Piazza, Jennifer M. Scalici, Luciana Madeira da Silva   +16 more
doaj   +2 more sources

PDE10A Inactivation Prevents Doxorubicin-Induced Cardiotoxicity and Tumor Growth. [PDF]

Circ Res, 2023
Background: Cyclic nucleotides play critical roles in cardiovascular biology and disease. PDE10A (phosphodiesterase 10A) is able to hydrolyze both cAMP and cGMP.
Chen S, Chen J, Du W, Mickelsen DM, Shi H, Yu H, Kumar S, Yan C.   +7 more
europepmc   +2 more sources