ArticleACS chemical neuroscience2015
Kinetic Analysis and Quantification of [¹¹C]Martinostat for in Vivo HDAC Imaging of the Brain.
Article in ACS chemical neuroscience, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers, 1 of them a synthesis that pooled it.
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Who cites it
34 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Radiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade.International journal of molecular sciences · 2022Pooled it
- PET neuroimaging reveals histone deacetylase dysregulation in schizophrenia.The Journal of clinical investigation · 2019Trial
- Insights into neuroepigenetics through human histone deacetylase PET imaging.Science translational medicine · 2016Trial
- Histone Modifications in Cardiovascular Disease: Mechanisms and Therapeutic Opportunities.MedComm · 2026Review
- Imaging brain class I histone deacetylase changes in the Lewy body dementias and Parkinson's disease.Clinical epigenetics · 2026Article
- Can Nuclear Imaging Detect Trained Immunity in Cardiovascular Disease?Arteriosclerosis, thrombosis, and vascular biology · 2026Review
- Preliminary Exploration of Pseudo-CT-Based Attenuation Correction for Simultaneous PET/MRI Brain Imaging in Nonhuman Primates.ACS omega · 2023Article
- Elaboration of the Effective Multi-Target Therapeutic Platform for the Treatment of Alzheimer's Disease Based on Novel Monoterpene-Derived Hydroxamic Acids.International journal of molecular sciences · 2023Article
- High-Contrast PET Imaging with [Journal of medicinal chemistry · 2023Article
- Introducing HDAC-Targeting Radiopharmaceuticals for Glioblastoma Imaging and Therapy.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Development of a potential PET probe for HDAC6 imaging in Alzheimer's disease.Acta pharmaceutica Sinica. B · 2022Article
- [Nature communications · 2022Article
- Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer [Pharmaceuticals (Basel, Switzerland) · 2022Article
- Design, synthesis, biochemical evaluation, radiolabeling and in vivo imaging with high affinity class-IIa histone deacetylase inhibitor for molecular imaging and targeted therapy.European journal of medicinal chemistry · 2022Article
- Novel late-stage radiosynthesis of 5-[18F]-trifluoromethyl-1,2,4-oxadiazole (TFMO) containing molecules for PET imaging.Scientific reports · 2021Article
- Epigenetic Targeting of Histone Deacetylases in Diagnostics and Treatment of Depression.International journal of molecular sciences · 2021Review
- Imaging Epigenetics of Prenatal THC.ACS chemical neuroscience · 2021Article
- Clinical validation of the novel HDAC6 radiotracer [European journal of nuclear medicine and molecular imaging · 2021Article
- PET imaging of glucose and fatty acid metabolism for NAFLD patients.Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology · 2020Article
- Molecular and Imaging Biomarkers in Alzheimer's Disease: A Focus on Recent Insights.Journal of personalized medicine · 2020Review
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Epigenetic mechanisms mediated by histone deacetylases (HDACs) have been implicated in a wide-range of CNS disorders and may offer new therapeutic opportunities. In vivo evaluation of HDAC density and drug occupancy has become possible with [(11)C]Martinostat, which exhibits selectivity for a subset of class I/IIb HDAC enzymes. In this study, we characterize the kinetic properties of [(11)C]Martinostat in the nonhuman primate (NHP) brain in preparation for human neuroimaging studies. The goal of this work was to determine whether classic compartmental analysis techniques were appropriate and to further determine if arterial plasma is required for future NHP studies. Using an arterial plasma input function, several analysis approaches were evaluated for robust outcome measurements. [(11)C]Martinostat showed high baseline distribution volume (VT) ranging from 29.9 to 54.4 mL/cm(3) in the brain and large changes in occupancy (up to 99%) with a blocking dose approaching full enzyme saturation. An averaged nondisplaceable tissue uptake (VND) of 8.6 ± 3.7 mL/cm(3) suggests high specific binding of [(11)C]Martinostat. From a two-tissue compartment model, [(11)C]Martinostat exhibits a high K1 (averaged K1 of 0.65 mL/cm(3)/min) and a small k4 (average of 0.0085 min(-1)). Our study supports that [(11)C]Martinostat can be used to detect changes in HDAC density and occupancy in vivo and that simplified analysis not using arterial blood could be appropriate.
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