LY404039

LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms). It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications. LY404039 inhibits the binding of domperidone (Cay-18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor. LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.Formal Name: (1R,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide. CAS Number: 635318-11-5. Molecular Formula: C7H9NO6S. Formula Weight: 235.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 0.5 mg/mL. SMILES: O=S1([C@]([C@@H]2C(O)=O)([H])[C@]2([H])[C@@](C(O)=O)(N)C1)=O. InChi Code: InChI=1S/C7H9NO6S/c8-7(6(11)12)1-15(13,14)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1. InChi Key: AVDUGNCTZRCAHH-MDASVERJSA-N.