An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction

Bioorganic & Medicinal Chemistry Letters
Stephen P EastKai Gerlach

Abstract

A high-throughput screening campaign identified 4-((E)-styryl)-pyrimidin-2-ylamine (11) as a positive allosteric modulator of the metabotropic glutamate (mGlu) receptor subtype 4. An evaluation of the structure-activity relationships (SAR) of 11 is described and the efficacy of this compound in a haloperidol-induced catalepsy rat model following oral administration is presented.

References

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Citations

Jun 22, 2011·Journal of Medicinal Chemistry·Sang-Phyo HongDarío Doller
Feb 14, 2016·Journal of Neuroimmune Pharmacology : the Official Journal of the Society on NeuroImmune Pharmacology·Ranjani PonnazhaganDavid G Standaert
Nov 15, 2013·Journal of Neurochemistry·Claire J Williams, David T Dexter
Oct 1, 2013·Neurobiology of Disease·Hilary Highfield Nickols, P Jeffrey Conn
Aug 9, 2019·Current Topics in Medicinal Chemistry·Zoltán OrgovánGyörgy M Keserű
Jul 21, 2020·ChemMedChem·Zoltán OrgovánGyörgy M Keserű
Apr 28, 2017·Molecular Brain·James MaksymetzP Jeffrey Conn
Mar 27, 2018·Neuropharmacology·Delphine Charvin
Apr 6, 2021·The European Journal of Neuroscience·Isabelle WakuAmanda R de Oliveira

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