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LY 341495Cat. No. 1209 |
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Chemical Name: (2S)-2-Amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid |
Biological Activity
Highly potent and selective group II metabotropic glutamate receptor antagonist (Ki/IC50 values 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. Disodium salt (Cat. No. 4062) also available. Also available as part of the Group II mGlu Receptor Tocriset™, Group III mGlu Receptor Tocriset™ and Mixed mGlu Receptor Tocriset™.Licensing Information
Sold with the permission of Eli Lilly and CompanyCertificate of Analysis / Safety Data Sheet
References
Fitzjohn et al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology 37 1445. PMID: 9886667.
Kingston et al (1998) LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology 37 1. PMID: 9680254.
Ornstein et 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. PMID: 9464367.
Johnson et 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. PMID: 10530814.
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