现货，LY404039，selleck，美国进口，mGluR YZ剂，CAS号: 635318-11-5，目录号 S6001

LY404039 is a selective metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3 agonist with Ki of 149 and 92nM for mGlu2 and mGlu3, respectively.Functional activity of LY404039 at group II and group III mGlu receptors is measured by the inhibition of forskolin-stimulated cAMP formation. It is nanomolar potent agonists at human mGlu2 and mGlu3 receptors, as indicated by the inhibition of forskolin-stimulated cAMP formation (LY404039: mGlu2, EC50 =23 nM; mGlu3, EC50 = 48 nM). It suppressed the frequency of 5-HT-induced EPSCs with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM. Intraperitoneal administration of LY404039 (10 mg/kg) to wild-type mice significantly inhibited increases evoked by PCP (7.5 mg/kg) in ambulations. It produced a dose-dependent reduction of increases evoked by AMP (5 mg/kg) in ambulations. ^[1][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, Bryan G. Johnson,et al. JPET 2007;321:308–317
• Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039) Matthew J. Fell, Kjell A. Svensson,et al. JPET 2008;326:209–217

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