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

  • Bioorg Med Chem Lett. 2010 Aug 15;20(16):4901-5. doi: 10.1016/j.bmcl.2010.06.078.
Stephen P East  1 ,  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
Affiliations
PMID: 20638279 DOI: 10.1016/j.bmcl.2010.06.078
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.

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