Abstract |
A series of 2-methoxyacylhydrazones were optimized to yield compounds with high affinity for PDE10A. Several compounds demonstrated efficacy in animal models of schizophrenia, including conditioned avoidance response and a pro-psychotic phencyclidine hyperactivity model.
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Authors | Neil S Cutshall, Rene Onrust, Alex Rohde, Sasha Gragerov, Lauren Hamilton, Kevin Harbol, Hui-Rong Shen, Shawn McKee, Charles Zuta, Galina Gragerova, Vince Florio, Thomas N Wheeler, Jennifer L Gage |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 22
Issue 17
Pg. 5595-9
(Sep 01 2012)
ISSN: 1464-3405 [Electronic] England |
PMID | 22841436
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2012 Elsevier Ltd. All rights reserved. |
Chemical References |
- Antipsychotic Agents
- Hydrazones
- Phosphodiesterase Inhibitors
- Pde10a protein, mouse
- Phosphoric Diester Hydrolases
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Topics |
- Animals
- Antipsychotic Agents
(chemistry, pharmacokinetics, therapeutic use)
- Hydrazones
(chemistry, pharmacokinetics, therapeutic use)
- Mice
- Phosphodiesterase Inhibitors
(chemistry, pharmacokinetics, therapeutic use)
- Phosphoric Diester Hydrolases
(metabolism)
- Schizophrenia
(drug therapy, enzymology)
- Structure-Activity Relationship
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