2. Academic Validation
  3. 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists

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

Affiliation

  • 1 Eli Lilly and Company Ltd, Lilly Research Centre, Windlesham, Surrey, UK. baker_s_richard@lilly.com
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.

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