Results 41 to 50 of about 4,657 (257)

Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia

Journal of Medicinal Chemistry, 2023
PDE10A is an important regulator of striatal signaling that, when inhibited, can normalize dysfunctional activity. Given the involvement of dysfunctional striatal activity with schizophrenia, PDE10A inhibition represents a potentially novel means for its
M. E. Layton, J. Kern, Timothy J. Hartingh, W. Shipe, I. Raheem, M. Kandebo, R. Hayes, Sarah L. Huszar, Donnie M Eddins, B. Ma, J. Fuerst, G. Wollenberg, Jing Li, Jeff Fritzen, G. McGaughey, J. Uslaner, Sean M. Smith, P. Coleman, Christopher D. Cox   +18 more
semanticscholar   +1 more source

Papaverine, a phosphodiesterase 10A inhibitor, ameliorates quinolinic acid-induced synaptotoxicity in human cortical neurons [PDF]

, 2021
Phosphodiesterase-10A (PDE10A) hydrolyse the secondary messengers cGMP and cAMP, two molecules playing important roles in neurodevelopment and brain functions.
Basappa, S., Bhat, Abid, Chidambaram, Saravana B., Chow, Sharron, Essas, Musthafa M., Guillemin, Gilles J., Heng, Benjamin, Tan, Vanessa   +7 more
core   +1 more source

Discovery of a highly specific 18F-labeled PET ligand for phosphodiesterase 10A enabled by novel spirocyclic iodonium ylide radiofluorination

Acta Pharmaceutica Sinica B, 2022
As a member of cyclic nucleotide phosphodiesterase (PDE) enzyme family, PDE10A is in charge of the degradation of cyclic adenosine (cAMP) and guanosine monophosphates (cGMP). While PDE10A is primarily expressed in the medium spiny neurons of the striatum,
Zhiwei Xiao, Huiyi Wei, Yi Xu, Ahmed Haider, Junjie Wei, Shiyu Yuan, Jian Rong, Chunyu Zhao, Guocong Li, Weibin Zhang, Huangcan Chen, Yuefeng Li, Lingling Zhang, Jiyun Sun, Shaojuan Zhang, Hai-Bin Luo, Sen Yan, Qijun Cai, Lu Hou, Chao Che, Steven H. Liang, Lu Wang   +21 more
doaj   +1 more source

Abrupt and Severe Onset of Dystonia, Chorea and Hemiplegic Episodes in a Young Boy with a Novel Heterozygous Missense Variant in the GTPase Domain of RHOBTB2. [PDF]

Mov Disord Clin Pract
Movement Disorders Clinical Practice, Volume 12, Issue S2, Page S13-S15, August 2025.
Hoang PT, Bledsoe IO, San Luciano M.
europepmc   +2 more sources

Effects of PDE10A inhibitor MK-8189 in people with an acute episode of schizophrenia: A randomized proof-of-concept clinical trial

Schizophrenia Research
Yuki Mukai, Robert Lupinacci, Stephen R. Marder, Linda Snow‐Adami, Tiffini Voss, Sean M. Smith, Michael Egan   +6 more
openalex   +2 more sources

Biallelic Mutations in PDE10A Lead to Loss of Striatal PDE10A and a Hyperkinetic Movement Disorder with Onset in Infancy [PDF]

The American Journal of Human Genetics, 2016
Deficits in the basal ganglia pathways modulating cortical motor activity underlie both Parkinson disease (PD) and Huntington disease (HD). Phosphodiesterase 10A (PDE10A) is enriched in the striatum, and animal data suggest that it is a key regulator of this circuitry.
Christine A. Strick, Khanh Q. Nguyen, Veronica Reinhart, Katariina Mankinen, Jacek Majewski, Laura Huilaja, David T. Bonthron, Ian M. Carr, Tiina Hurskainen, John F. Harms, Jarkko Johansson, Christine P. Diggle, Hannaleena Kokkonen, Hannaleena Kokkonen, Matti Kallioinen, Larry C. James, Päivi Vieira, Kati Alakurtti, Karen Pysden, Somayyeh Fahiminiya, Saghira Malik Sharif, Christopher J. Schmidt, Tiago Reis Marques, Raija Sormunen, Raija Sormunen, Melanie Allen, Jan-Philip Schülke, Eija Anttila, Manju A. Kurian, Manju A. Kurian, Stacey J. Sukoff Rizzo, Christopher M. Watson, Michael Popiolek, Alexander F. Markham, Nicholas J. Brandon, Kaisa Tasanen, Michelle Vanase-Frawley, Oliver D. Howes, Oliver D. Howes, Johanna Uusimaa, Johanna Uusimaa, Marius Politis, Juha O. Rinne, Reetta Hinttala, Eamonn Sheridan, Erik I. Charych, Joanne Ng, Joanne Ng   +47 more
openaire   +8 more sources

Ibudilast Protects Retinal Bipolar Cells From Excitotoxic Retinal Damage and Activates the mTOR Pathway. [PDF]

Glia
Main Points Ibudilast, a MIF and PDE inhibitor, preserves the form and function of the retina, especially bipolar cells, during excitotoxic damage. Ibudilast upregulates multiple signaling pathways, including mTOR, in damaged Müller glia and bipolar cells.
Hamadmad S, Heisler-Taylor T, Goswami S, Hawthorn E, Chaurasia S, Martini D, Summitt D, Zatari A, Shalash R, Sohail M, Urbanski EG, Bernstein K, Racine J, Satoskar A, El-Hodiri HM, Fischer AJ, Cebulla CM.   +16 more
europepmc   +2 more sources

Inhibition of PDE10A-Rescued TBI-Induced Neuroinflammation and Apoptosis through the cAMP/PKA/NLRP3 Pathway

Evidence-Based Complementary and Alternative Medicine, 2022
Phosphodiesterase 10A (PDE10A) is a dual-substrate phosphodiesterase that is highly expressed in the striatal complex. PDE10A is an important target for the treatment of ganglion dysfunction and neuroinflammation-related diseases, but its possible impact
Jin Huang, Dang Tang, Yiqiang Cao, Yonggang Wang, Jiang Long, Lingxiang Wei, Hai Song   +6 more
semanticscholar   +1 more source

Striatal phosphodiesterase 10A availability is altered secondary to chronic changes in dopamine neurotransmission

EJNMMI Radiopharmacy and Chemistry, 2016
Background Phosphodiesterase 10A (PDE10A) is an important regulator of nigrostriatal dopamine (DA) neurotransmission. However, little is known on the effect of alterations in DA neurotransmission on PDE10A availability. Here, we used [18F]JNJ42259152 PET
Maarten Ooms, Sofie Celen, Ronald De Hoogt, Ilse Lenaerts, Johnny Liebregts, Greet Vanhoof, Xavier Langlois, Andrey Postnov, Michel Koole, Alfons Verbruggen, Koen Van Laere, Guy Bormans   +11 more
doaj   +1 more source

Comparison of [11C]TZ1964B and [18F]MNI659 for PET imaging brain PDE10A in nonhuman primates [PDF]

, 2016
Phosphodiesterase 10A (PDE10A) inhibitors show therapeutic effects for diseases with striatal pathology. PET radiotracers have been developed to quantify in vivo PDE10A levels and target engagement for therapeutic interventions. The aim of this study was
Alagille, David, Flores, Hubert, Han, Junbin, Jin, Hongjun, Liu, Hui, Perlmutter, Joel S, Su, Yi, Tamagnan, Gilles, Tu, Zhude, Yang, Hao, Yue, Xuyi   +10 more
core   +2 more sources