See today's edition of
DailyUpdates in your
therapeutic area
Search all articles

Keywords:

Boolean terms AND, OR, NOT can be used. Phrases should be entered within quotes. For wildcards use an *

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

Bioorganic & medicinal chemistry letters 2010 Jun 25; In press

Link to PubMed abstract

East S SP, Bamford S, Dietz M MG, Eickmeier C, Flegg A, Ferger B, Gemkow M MJ, Heilker R, Hengerer B, Kotey A, Loke P, Schänzle G, Schubert H HD, Scott J, Whittaker M, Williams M, Zawadzki P, Gerlach K

Evotec (UK) Ltd, 114 Milton Park, Abingdon, OX14 4SD, UK.

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.

Keywords: motor dysfunction mGlu4