Novel 2-methoxyacylhydrazones as potent, selective PDE10A inhibitors with activity in animal models of schizophrenia

Autor:	Lauren Hamilton, Rene Onrust, Thomas Neil Wheeler, Charles Prince Zuta, Sasha Gragerov, Alex Rohde, Shawn McKee, Neil S. Cutshall, Jennifer Lynn Gage, Vince Florio, Harbol Kevin L, Galina Gragerova, Hui-Rong Shen
Rok vydání:	2012
Předmět:	Phosphodiesterase Inhibitors Clinical Biochemistry Pharmaceutical Science Pharmacology Avoidance response Biochemistry Mice Structure-Activity Relationship Drug Discovery medicine Animal models of schizophrenia Structure–activity relationship Animals Molecular Biology Phencyclidine biology Chemistry Phosphoric Diester Hydrolases Organic Chemistry Hydrazones Phosphodiesterase medicine.disease Schizophrenia Enzyme inhibitor biology.protein Molecular Medicine PDE10A medicine.drug Antipsychotic Agents
Zdroj:	Bioorganicmedicinal chemistry letters. 22(17)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d86d367c4f6331c08078f09eadeaaf6b https://pubmed.ncbi.nlm.nih.gov/22841436 Zobrazit plný text záznamu Full Text from ScienceDirect