现货,LY2140023 (LY404039) ,CAS号: 635318-11-5 ,美国进口, 神经信号通路(Neuronal Signaling) , mGluR,mGluR 抑制剂,selleck,S6001

信号转导通路: 神经信号通路(Neuronal Signaling) >> mGluR >> mGluR 抑制剂 >> LY2140023 (LY404039)http://selleck.cn/ly2140023-ly404039-S6001.html

技术数据:

分子量(MW): 235.22

化学式:

C7H9NO6S

溶解度: DMSO ≥1mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 635318-11-5

生物活性

 

LY2140023 (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 LY2140023 (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 LY2140023 (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]

 

参考文献

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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