4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists

  • Bioorg Med Chem Lett. 2000 Aug 21;10(16):1807-10. doi: 10.1016/s0960-894x(00)00346-2.
S R Baker  1 ,  D Bleakman ,  J Ezquerra ,  B A Ballyk ,  M Deverill ,  K Ho ,  R K Kamboj ,  I Collado ,  C Domínguez ,  A Escribano ,  A I Mateo ,  C Pedregal ,  A Rubio
Affiliations
  • 1. Eli Lilly and Company Ltd, Lilly Research Centre, Windlesham, Surrey, UK. [email protected]
PMID: 10969973 DOI: 10.1016/s0960-894x(00)00346-2
Abstract

Twenty-four 4-alkylidene glutamic acids were synthesised and tested as potential subtype selective GluR5 and 6 ligands. It was found that a critical size of alkylidene group gave potent and selective GluR5 receptor agonists. LY339624 had Kis of 0.0326 and >100 microM on GluR5 and 6 receptors, respectively.