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Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis)
Cyclic adenosine monophosphate (cAMP) signalling plays an important role in synaptic plasticity and information processing in the hippocampal and basal ganglia systems. The augmentation of cAMP signalling through the selective inhibition of phosphodiesterases represents a viable strategy to treat di...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106781/ https://www.ncbi.nlm.nih.gov/pubmed/25050979 http://dx.doi.org/10.1371/journal.pone.0102449 |
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author | Sutcliffe, Jane S. Beaumont, Vahri Watson, James M. Chew, Chang Sing Beconi, Maria Hutcheson, Daniel M. Dominguez, Celia Munoz-Sanjuan, Ignacio |
author_facet | Sutcliffe, Jane S. Beaumont, Vahri Watson, James M. Chew, Chang Sing Beconi, Maria Hutcheson, Daniel M. Dominguez, Celia Munoz-Sanjuan, Ignacio |
author_sort | Sutcliffe, Jane S. |
collection | PubMed |
description | Cyclic adenosine monophosphate (cAMP) signalling plays an important role in synaptic plasticity and information processing in the hippocampal and basal ganglia systems. The augmentation of cAMP signalling through the selective inhibition of phosphodiesterases represents a viable strategy to treat disorders associated with dysfunction of these circuits. The phosphodiesterase (PDE) type 4 inhibitor rolipram has shown significant pro-cognitive effects in neurological disease models, both in rodents and primates. However, competitive non-isoform selective PDE4 inhibitors have a low therapeutic index which has stalled their clinical development. Here, we demonstrate the pro-cognitive effects of selective negative allosteric modulators (NAMs) of PDE4D, D159687 and D159797 in female Cynomolgous macaques, in the object retrieval detour task. The efficacy displayed by these NAMs in a primate cognitive task which engages the corticostriatal circuitry, together with their suitable pharmacokinetic properties and safety profiles, suggests that clinical development of these allosteric modulators should be considered for the treatment of a variety of brain disorders associated with cognitive decline. |
format | Online Article Text |
id | pubmed-4106781 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-41067812014-07-23 Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) Sutcliffe, Jane S. Beaumont, Vahri Watson, James M. Chew, Chang Sing Beconi, Maria Hutcheson, Daniel M. Dominguez, Celia Munoz-Sanjuan, Ignacio PLoS One Research Article Cyclic adenosine monophosphate (cAMP) signalling plays an important role in synaptic plasticity and information processing in the hippocampal and basal ganglia systems. The augmentation of cAMP signalling through the selective inhibition of phosphodiesterases represents a viable strategy to treat disorders associated with dysfunction of these circuits. The phosphodiesterase (PDE) type 4 inhibitor rolipram has shown significant pro-cognitive effects in neurological disease models, both in rodents and primates. However, competitive non-isoform selective PDE4 inhibitors have a low therapeutic index which has stalled their clinical development. Here, we demonstrate the pro-cognitive effects of selective negative allosteric modulators (NAMs) of PDE4D, D159687 and D159797 in female Cynomolgous macaques, in the object retrieval detour task. The efficacy displayed by these NAMs in a primate cognitive task which engages the corticostriatal circuitry, together with their suitable pharmacokinetic properties and safety profiles, suggests that clinical development of these allosteric modulators should be considered for the treatment of a variety of brain disorders associated with cognitive decline. Public Library of Science 2014-07-22 /pmc/articles/PMC4106781/ /pubmed/25050979 http://dx.doi.org/10.1371/journal.pone.0102449 Text en © 2014 munoz-sanjuan et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited. |
spellingShingle | Research Article Sutcliffe, Jane S. Beaumont, Vahri Watson, James M. Chew, Chang Sing Beconi, Maria Hutcheson, Daniel M. Dominguez, Celia Munoz-Sanjuan, Ignacio Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) |
title | Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) |
title_full | Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) |
title_fullStr | Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) |
title_full_unstemmed | Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) |
title_short | Efficacy of Selective PDE4D Negative Allosteric Modulators in the Object Retrieval Task in Female Cynomolgus Monkeys (Macaca fascicularis) |
title_sort | efficacy of selective pde4d negative allosteric modulators in the object retrieval task in female cynomolgus monkeys (macaca fascicularis) |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106781/ https://www.ncbi.nlm.nih.gov/pubmed/25050979 http://dx.doi.org/10.1371/journal.pone.0102449 |
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