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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1019-22. doi: 10.1016/j.bmcl.2011.11.127. Epub 2011 Dec 9.

The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.

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  • 1Department of Medicinal Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, USA.;


High-throughput screening identified a series of pyrazoloquinolines as PDE10A inhibitors. The SAR development led to the discovery of compound 27 as a potent, selective, and orally active PDE10A inhibitor. Compound 27 inhibits MK-801 induced hyperactivity at 3mg/kg with an ED(50) of 4mg/kg and displays a ∼6-fold separation between the ED(50) for inhibition of MK-801 induced hyperactivity and hypolocomotion in rats.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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