货号 | 18408-1mg |
描述 | 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).1 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.1 LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.2 LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.3 |
供应商 | Cayman |
应用文献 | |
1.Rorick-Kehn, L.M.,Johnson, B.G.,Burkey, J.L., et al. 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). J. Pharmacol. Exp. Ther. 321(1), 308-317 (2007). 2.Seeman, P., and Guan, H.C. Glutamate agonist LY404,039 for treating schizophrenia has affinity for the dopamine D2(High) receptor. Synapse 63(10), 935-939 (2009). 3.Rorick-Kehn, L.M.,Johnson, B.G.,Knitowski, K.M., et al. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders. Psychopharmacology (Berl) 193(1), 121-136 (2007). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 235.2 |
分子式 | C7H9NO6S |
CAS号 | 635318-11-5 |
稳定性 | ≥ 2 years |
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