ArticleFrontiers in molecular neuroscience2017
The Phosphodiesterase 10A Inhibitor PF-2545920 Enhances Hippocampal Excitability and Seizure Activity Involving the Upregulation of GluA1 and NR2A in Post-synaptic Densities.
Article in Frontiers in molecular neuroscience, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 24 citations in OpenAlex.
- Novel Phosphodiesterase‑2 Inhibitors Discovered via Structure-Based Virtual Screening Targeting the Allosteric GAF‑B Domain.ACS medicinal chemistry letters · 2026Article
- cGAS-mediated type I IFN signaling contributes to disease progression in drug-refractory epilepsy.Nature neuroscience · 2026Article
- cGAS-mediated IFN-I signaling contributes to disease progression in drug-refractory epilepsy.bioRxiv : the preprint server for biology · 2026Article
- An integrated single-nucleus and spatial transcriptomics atlas reveals the molecular landscape of the human hippocampus.Nature neuroscience · 2025Article
- Cyclic nucleotide phosphodiesterases as drug targets.Pharmacological reviews · 2025Review
- PDE10A as a novel diagnostic and therapeutic target in cancer: insights and challenges.Frontiers in oncology · 2025Review
- An integrated single-nucleus and spatial transcriptomics atlas reveals the molecular landscape of the human hippocampus.bioRxiv : the preprint server for biology · 2024Article
- THPP-1 PDE10A inhibitor reverses the cognitive deficits and hyperdopaminergic state in a neurodevelopment model of schizophrenia.Schizophrenia research · 2024Article
- The Traf2 and NcK interacting kinase inhibitor NCB-0846 suppresses seizure activity involving the decrease of GRIA1.Genes & diseases · 2024Article
- PGC-1α Affects Epileptic Seizures by Regulating Mitochondrial Fusion in Epileptic Rats.Neurochemical research · 2023Article
- Inhibition of PDE10A-Rescued TBI-Induced Neuroinflammation and Apoptosis through the cAMP/PKA/NLRP3 Pathway.Evidence-based complementary and alternative medicine : eCAM · 2022Article
- The CBInternational journal of molecular sciences · 2021Review
- Aspects of cAMP Signaling in Epileptogenesis and Seizures and Its Potential as Drug Target.Neurochemical research · 2020Review
- Genome-Wide Association of Genetic Variants With Refraction, Axial Length, and Corneal Curvature: A Longitudinal Study of Chinese Schoolchildren.Frontiers in genetics · 2020Article
- Spatiotemporal Expression of SphK1 and S1PR2 in the Hippocampus of Pilocarpine Rat Model and the Epileptic Foci of Temporal Lobe Epilepsy.Frontiers in cell and developmental biology · 2020Article
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11 authors at 3 institutions in 1 country.
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Abstract
Phosphodiesterase regulates the homeostasis of cAMP and cGMP, which increase the strength of excitatory neural circuits and/or decrease inhibitory synaptic plasticity. Abnormally, synchronized synaptic transmission in the brain leads to seizures. A phosphodiesterase 10A (PDE10A) inhibitor PF-2545920 has recently attracted attention as a potential therapy for neurological and psychiatric disorders. We hypothesized that PF-2545920 plays an important role in status epilepticus (SE) and investigated the underlying mechanisms. PDE10A was primarily located in neurons, and PDE10A expression increased significantly in patients with temporal lobe epilepsy. PF-2545920 enhanced the hyperexcitability of pyramidal neurons in rat CA1, as measured by the frequency of action potentials and miniature excitatory post-synaptic current. GluA1 and NR2A expression also increased significantly in post-synaptic densities, with or without SE in rats treated with PF-2545920. The ratio of
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