4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.
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.
Baker
S R
SR
Eli Lilly and Company Ltd, Lilly Research Centre, Windlesham, Surrey, UK. baker_s_richard@lilly.com
Bleakman
D
D
Ezquerra
J
J
Ballyk
B A
BA
Deverill
M
M
Ho
K
K
Kamboj
R K
RK
Collado
I
I
Domínguez
C
C
Escribano
A
A
Mateo
A I
AI
Pedregal
C
C
Rubio
A
A
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
D008024:Ligands; D011761:Pyrrolidonecarboxylic Acid; D018092:Kainic Acid Receptors; D000097806:GluK2 Kainate Receptor