Chemical Name:(2S)-2-Amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xan
th-9-yl) propanoic acid
Biological Activity:
Highly potent and selective group II
metabotropic glutamate receptor antagonist (Ki/IC50values are 2.3, 1.3, 173, 990, 6800, 8200
and 22000 nM for human mGlu2, mGlu3, mGlu8, mGlu7a, mGlu1a,
mGlu5a and mGlu4a receptors respectively). Readily brain
penetrant and active in vivo.
Ornsteinet al (1998) 2-Substituted
(2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl) glycines as potent and
selective antagonists of group II metabotropic glutamate receptors. 2. Effects
of aromatic substitution, pharmacological characterization, and bioavailability.
J.Med.Chem. 41 358. Kingstonet al (1998) LY341495
is a nanomolar potent and selective antagonist of group II metabotropic
glutamate receptors. Neuropharmacology 37 1. Fitzjohnet
al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for
both cloned and novel mGlu receptors in hippocampal synaptic plasticity.
Neuropharmacology 37 1445. Johnsonet al (1999) [3H]-LY341495 as a novel
antagonist radioligand for group II metabotropic glutamate receptors:
characterization of binding to membranes of mGlu receptor subtype expressing
cells. Neuropharmacology 38 1519.
