Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.

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作者： Susana,Conde-Ceide ^[1] ; Jesús,Alcázar ^[1] ; Sergio A,Alonso de Diego ^[1] ; Silvia,López ^[1] ; María Luz,Martín-Martín ^[1] ; Carlos M,Martínez-Viturro ^[1] ; Miguel-Angel,Pena ^[1] ; Han Min,Tong ^[1] ; Hilde,Lavreysen ^[2] ; Claire,Mackie ^[3] ; Thomas M,Bridges ^[4] ; J Scott,Daniels ^[4] ; Colleen M,Niswender ^[4] ; Carrie K,Jones ^[4] ; Gregor J,Macdonald ^[2] ; Thomas,Steckler ^[2] ; P Jeffrey,Conn ^[4] ; Shaun R,Stauffer ^[4] ; Craig W,Lindsley ^[5] ; José Manuel,Bartolomé-Nebreda ^[6]

作者单位： Neuroscience Medicinal Chemistry, Janssen Research and Development, Jarama 75A, 45007 Toledo, Spain. ^[1] Neuroscience, Janssen Research and Development, Turnhoutseweg 30, B-2340 Beerse, Belgium. ^[2] Discovery Sciences ADME/Tox, Janssen Research and Development, Turnhoutseweg 30, B-2340 Beerse, Belgium. ^[3] Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA. ^[4] Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA. Electronic address: craig.lindsley@vanderbilt.edu. ^[5] Neuroscience Medicinal Chemistry, Janssen Research and Development, Jarama 75A, 45007 Toledo, Spain. Electronic address: jbartolo@its.jnj.com. ^[6]

关键词 Metabotropic glutamate receptor N-Methyl-d-aspartate (NMDA)Positive allosteric modulator (PAM)Schizophrenia mGlu(5)