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Novel 2-methoxyacylhydrazones as potent, selective PDE10A inhibitors with activity in animal models of schizophrenia |
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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 |
| Affiliation: | Omeros Corp., 1420 Fifth Ave, Suite 2600, Seattle, WA 98101, USA. |
| 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. |
| Keywords: | PDE10 PDE10A Phosphodiesterase Schizophrenia Hydrazone Hydrazide PDE Enzyme inhibitor Cognitive |
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