Chemical Name:(1R,4R,5S,6R)-4-Amino-2-oxabicyclo[3.1.0]hexane-4,6-dic
arboxylic acid
Biological Activity:
Highly selective group II mGlu receptor agonist
(EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3
respectively) that displays > 80-fold selectivity over group I and group III
receptors. Provides protection against NMDA-mediated cell death in vitro and
offers almost complete protection against CA1 hippocampal damage following
global ischaemia in gerbils. Orally and systemically active.
Bondet al (1999)
LY379268, a potent and selective group II metabotropic glutamate receptor
agonist, is neuroprotective in gerbil global, but not focal cerebral ischaemia.
Neurosci.Lett. 273 191. Bondet al (2000)
Neuroprotective effects of LY237268, a selective mGlu2/3 receptor agonist:
investigations into possible mechanisms of action in vivo.
J.Pharmacol.Exp.Ther. 294 800. Colladoet al (2002)
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl)
glycine is a potent and selective metabotropic group 2 agonist with anxiolytic
properties. J.Med.Chem. 45 3619.
