title: 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.
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.
authors.affiliation: Eli Lilly and Company Ltd, Lilly Research Centre, Windlesham, Surrey, UK. baker_s_richard@lilly.com
authors.forename: S R
authors.initials: SR
authors.lastname: Baker
authors.forename: D
authors.initials: D
authors.lastname: Bleakman
authors.forename: J
authors.initials: J
authors.lastname: Ezquerra
authors.forename: B A
authors.initials: BA
authors.lastname: Ballyk
authors.forename: M
authors.initials: M
authors.lastname: Deverill
authors.forename: K
authors.initials: K
authors.lastname: Ho
authors.forename: R K
authors.initials: RK
authors.lastname: Kamboj
authors.forename: I
authors.initials: I
authors.lastname: Collado
authors.forename: C
authors.initials: C
authors.lastname: Domínguez
authors.forename: A
authors.initials: A
authors.lastname: Escribano
authors.forename: A I
authors.initials: AI
authors.lastname: Mateo
authors.forename: C
authors.initials: C
authors.lastname: Pedregal
authors.forename: A
authors.initials: A
authors.lastname: Rubio
mesh_terms: D000818:Animals; D002460:Cell Line; D002478:Cells, Cultured; D005727:Ganglia, Spinal / Q000166:cytology; D006801:Humans; D007668:Kidney / Q000166:cytology / Q000196:embryology; D008024:Ligands; D015394:Molecular Structure; D009475:Neurons, Afferent / Q000378:metabolism; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018092:Kainic Acid Receptors / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship; D000097806:GluK2 Kainate Receptor
chemical_list: D008024:Ligands; D011761:Pyrrolidonecarboxylic Acid; D018092:Kainic Acid Receptors; D000097806:GluK2 Kainate Receptor