Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2).
This article describes recent medicinal chemistry progress toward selective potentiators of the metabotropic glutamate receptor 2 (mGluR2). Groups at Lilly and Merck have identified new classes of potentiators that exhibit selectivity for mGluR2 over the seven other subtypes of mGluRs. Structure-activity relationships as well as pharmacokinetic properties and in vivo activity are reviewed.
Rudd
Michael T
MT
Department of Medicinal Chemistry, Merck Research Laboratories, WP14-3, Merck & Co., Inc., PO Box 4, West Point, PA 19486 USA.
McCauley
John A
JA
D000494:Allosteric Regulation; D000818:Animals; D015195:Drug Design; D018690:Excitatory Amino Acid Agonists / Q000493:pharmacokinetics* / Q000494:pharmacology*; D006801:Humans; D018094:Receptors, Metabotropic Glutamate / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D018690:Excitatory Amino Acid Agonists; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2