Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator

A Ritzén, R Sindet, M Hentzer, N Svendsen…

Index: Ritzen, Andreas; Sindet, Rikke; Hentzer, Morten; Svendsen, Nannette; Brodbeck, Robbin M.; Bundgaard, Christoffer Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 12 p. 3275 - 3278

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Citation Number: 24

Abstract

Glutamate is the principal excitatory neurotransmitter in the mammalian central nervous system, and it mediates its effects through interaction with ionotropic and metabotropic receptors. The metabotropic glutamate receptors (mGluRs) are class C GPCRs and eight subtypes are known. They are divided into three groups based on their preferred G protein coupling and pharmacological responses to various ligands: Group I consisting of mGluR1 and ...