Results 211 to 220 of about 4,657 (257)
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Immunohistochemical localization of PDE10A in the rat brain
Brain Research, 2003PDE10A is a newly identified cAMP/cGMP phosphodiesterase for which mRNA is highly expressed in the mammalian striatum. In the present study, PDE10A protein and mRNA expression throughout the rat brain were determined, using a monoclonal antibody (24F3.F11) for Western blot and immunohistochemical analyses and an antisense riboprobe for in situ ...
David L Krull +13 more
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PDE10A Inhibitors: Novel Therapeutic Drugs for Schizophrenia
Current Pharmaceutical Design, 2011Disturbances of the basal ganglia processes is heavily involved in schizophrenia. Phosphodiesterase 10A (PDE10A) is a basal ganglia specific hydrolase, which plays an essential role in regulating cAMP/PKA and cGMP/PKG signalling cascades by controlling the magnitude, duration and cellular location of cAMP/cGMP elevation. Biochemical and behavioral data
Jacob Nielsen, Jan Kehler
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Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound
Bioorganic & Medicinal Chemistry Letters, 2012A series of pyrazoloquinolines, possessing (hetero)arylhydroxymethyl substituents at the quinoline C-4 position were evaluated as PDE10A inhibitors. Among these, methylpyrimidyl analogue 15 was identified as having good rodent and monkey exposure, and a MED of 10 mg/kg in an in vivo model.
Xiaoping Zhang +12 more
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Treating neuropsychiatric disorders with PDE10A inhibitors
Drug Discovery Today: Therapeutic Strategies, 2006Phosphodiesterase 10A (PDE10A) is a recently identified cyclic nucleotide phosphodiesterase expressed primarily in dopaminoreceptive medium spiny neurons of the striatum. This article provides a brief overview of the characterization, localization and function of this enzyme, the currently available pharmacological and genetic tools, and discusses ...
Christine A. Strick, Judith A. Siuciak
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Abstract 279: Role of PDE10A in Arterial Calcification
Arteriosclerosis, Thrombosis, and Vascular Biology, 2018Vascular calcification is highly prevalent in patients with diabetes mellitus and chronic kidney disease. When located in the media, arterial calcification is strongly associated with increased cardiovascular morbidity and mortality.
Tonghui Lin +3 more
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Circulation
Heart failure is a leading cause of death in the United States, and is associated with significant myocardial deterioration. cAMP and cGMP play critical roles in cardiovascular biology and disease.
Si Chen +5 more
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Heart failure is a leading cause of death in the United States, and is associated with significant myocardial deterioration. cAMP and cGMP play critical roles in cardiovascular biology and disease.
Si Chen +5 more
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PET Radioligands for imaging of the PDE10A in human: current status
Neuroscience Letters, 2019The development of β+ emitter tracers labelled with carbon-11 or fluorine-18 having optimal characteristics of affinity and selectivity for the phosphodiesterase 10 A protein has received considerable attention, due to the major implication of this enzyme in neurological and psychiatric disorders, such as Hungtington's disease, Parkinson's disease and ...
Giulia Boscutti +2 more
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Patented PDE10A inhibitors: novel compounds since 2007
Expert Opinion on Therapeutic Patents, 2009PDE10A inhibition has generated much excitement as a potential novel mechanism for the treatment of the positive symptoms of schizophrenia. PDE10A is only '10 years old' as a drug discovery target since it was first discovered in 1999, and thus PDE10A is an example of the modern drug discovery paradigm demonstrating the highly increased speed by which ...
Jan Kehler, John Paul Kilburn
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Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors
Bioorganic & Medicinal Chemistry Letters, 2011Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity studies improved the initial micromolar potency which was found in the lead compound by a 100-fold identifying 5-(1H-benzoimidazol-2-ylmethylsulfanyl)-2-methyl-[1,2,4]triazolo[1,5-c]quinazoline, 42 (PDE10A IC(50)=12 nM) as the most potent ...
Morten Langgård +8 more
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ACS Chemical Biology, 2021
A challenge for sensors targeting specific enzymes of interest in their native environment for direct imaging is that they rationally exploit a highly selective fluorescent probe with a high binding affinity to provide real-time detection ...
Yuqi Gao +13 more
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A challenge for sensors targeting specific enzymes of interest in their native environment for direct imaging is that they rationally exploit a highly selective fluorescent probe with a high binding affinity to provide real-time detection ...
Yuqi Gao +13 more
semanticscholar +1 more source