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

✍ Scribed by Stephen P. East; Samantha Bamford; Matthias G.A. Dietz; Christian Eickmeier; Adam Flegg; Boris Ferger; Mark J. Gemkow; Ralf Heilker; Bastian Hengerer; Adrian Kotey; Pui Loke; Gerhard Schänzle; Hans-Dieter Schubert; John Scott; Mark Whittaker; Mildred Williams; Przemyslaw Zawadzki; Kai Gerlach

Book ID
104004553
Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
616 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis

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.

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