An orally bioavailable positive allosteric modulator of the mGlu(4) receptor with efficacy in an animal model of motor dysfunction

作者：East Stephen P^*; Bamford Samantha; Dietz Matthias G A; Eickmeier Christian; Flegg Adam; Ferger Boris; Gemkow Mark J; Heilker Ralf; Hengerer Bastian; Kotey Adrian; Loke Pui; Schaenzle Gerhard; Schubert Hans Dieter; Scott John; Whittaker Mark; Williams Mildred; Zawadzki Przemyslaw; Gerlach Kai

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(16): 4901-4905.

DOI：10.1016/j.bmcl.2010.06.078

• Allosteric modulator
• mGlu(4)
• Parkinson's disease
• Styryl pyrimidinyl amines

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.

• 出版日期2010-8-15