title: Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.
abstract: Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.
authors.affiliation: Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
authors.forename: Alice L
authors.initials: AL
authors.lastname: Rodriguez
authors.forename: Ya
authors.initials: Y
authors.lastname: Zhou
authors.forename: Richard
authors.initials: R
authors.lastname: Williams
authors.forename: C David
authors.initials: CD
authors.lastname: Weaver
authors.forename: Paige N
authors.initials: PN
authors.lastname: Vinson
authors.forename: Eric S
authors.initials: ES
authors.lastname: Dawson
authors.forename: Thomas
authors.initials: T
authors.lastname: Steckler
authors.forename: Hilde
authors.initials: H
authors.lastname: Lavreysen
authors.forename: Claire
authors.initials: C
authors.lastname: Mackie
authors.forename: José M
authors.initials: JM
authors.lastname: Bartolomé
authors.forename: Gregor J
authors.initials: GJ
authors.lastname: Macdonald
authors.forename: J Scott
authors.initials: JS
authors.lastname: Daniels
authors.forename: Colleen M
authors.initials: CM
authors.lastname: Niswender
authors.forename: Carrie K
authors.initials: CK
authors.lastname: Jones
authors.forename: P Jeffrey
authors.initials: PJ
authors.lastname: Conn
authors.forename: Craig W
authors.initials: CW
authors.lastname: Lindsley
authors.forename: Shaun R
authors.initials: SR
authors.lastname: Stauffer
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D005998:Glycine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; D013449:Sulfonamides; D005998:Glycine