2. Academic Validation
  3. An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction

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

Affiliation

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.

Figures
Products