Chemical Name : LY2140023/LY404039/
CAS : 635318-11-5
Synonyms: (1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide
Solubility:DMSO (10 mM)
Storage:-20C 2 years
LY2140023/LY404039 is a nanomolar potent agonist at recombinant human mGlu2 and mGlu3 receptors (Ki = 149 and 92, respectively) and in rat neurons expressing native mGlu2/3 receptors (Ki = 88). LY2140023/LY404039 is highly selective for mGlu2/3 receptors, showing more than 100-fold selectivity for these receptors, versus ionotropic glutamate receptors, glutamate transporters, and other receptors targeted by known anxiolytic and antipsychotic medications. IC50 to mGlu2 and mGlu3 are 23��1 and 48��10nM respectively. With an EC50=141 nM to EPSPs.
1. Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: A randomized Phase 2 clinical trial. Patil, S.T., Zhang, L., et al. 2007 Nature Medicine 13 (9), pp. 1102-1107 2. Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Metabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist ( )-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]- hexane-4,6-dicarboxylic Acid (LY404039). Linda M. Rorick-Kehn, et al. 2007 Journal of Pharmacology and Experimental Therapeutics 321 (1), pp. 308-317 3. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders. Rorick-Kehn, L.M., Johnson, B.G., et al. 2007 Psychopharmacology 193 (1), pp. 121-136