Discovery of “Molecular Switches” within a Series of mGlu5 Allosteric Ligands Driven by a “Magic Methyl” Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype

• Lisa Barbaro,
• Alice L. Rodriguez,
• Ashlyn N. Blevins,
• Jonathan W. Dickerson,
• Natasha Billard,
• Olivier Boutaud,
• Jerri L. Rook,
• Colleen M. Niswender,
• P.Jeffrey Conn,
• Darren W. Engers,
• Craig W. Lindsley

Affiliations

Lisa Barbaro

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Alice L. Rodriguez

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Ashlyn N. Blevins

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Jonathan W. Dickerson

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Natasha Billard

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Olivier Boutaud

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Jerri L. Rook

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Colleen M. Niswender

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

P.Jeffrey Conn

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Darren W. Engers

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States

Craig W. Lindsley

†Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee, United States