Chemical Name:(S)-(+)-a-Amino-4-carboxy-2-methylbenzeneacetic acid
Biological Activity:
A
selective mGlu1a receptor antagonist, with an IC50 value
of 8.8 μM for blockade of quisqualate-induced phosphoinositide
hydrolysis vs. > 100 μM for mGlu5a, and
negligible action on group II and III receptors.
Clarket al (1997) (+)-2-Methyl-4-carboxyphenylglycine (LY
367385) selectively antagonises metabotropic glutamate mGluR1 receptors.
Bioorg.Med.Chem.Lett. 7 2777. Salt and Turner (1998)
Reduction of sensory and metabotropic glutamate receptor responses in the
thalamus by the novel metabotropic glutamate receptor-1-selective antagonist
S-2-methyl-4-carboxy-phenylglycine. Neuroscience 85 655. Chapmanet al (1999) Anticonvulsant actions of LY 367385
((+)-methyl-4-carboxyphenylglycine), and AIDA
((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur.J.Pharmacol. 368
17. Brunoet al (1999) Neuroprotective activity of the potent and
selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4
carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum
antagonist with equal affinity for mGlu1a and mGlu5 receptors.
Neuropharmacology 38 199.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.
