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- Zheng,G.Z. etal.(2005) J.Med.Chem. 48, 7374.
- Zhu,C.Z. etal.(2008) Eur.J.Pharmacol. 580, 314.
AlomoneLabsA-794278 inhibitsmGluR1-mediatedCa2+ mobilizationinU2OScells.Dose-responseof A-794278 (#A-435)normalizedinhibitionofhumanmGluR1-mediated,L-glutamate-evokedCa2+ mobilization.Cellswereloadedwithcalcium-sensitivedye,incubatedwitharangeofA-794278concentrations,andstimulatedwith5µML-glutamate(EC80).ChangesinintracellularCa2+ followingstimulationweredetectedaschangesinmaximumrelativefluorescence(RLU)usingFLIPRTETRA™.IC50 wasdeterminedat4.16nM.
- 1.Zheng,G.Z. etal.(2005) J.Med.Chem. 48, 7374.
- 2.Zhu,C.Z. etal.(2008) Eur.J.Pharmacol. 580, 314.
A-794278isapotent,non-competitiveantagonistofmGluR1.ItisatriazafluorenonederivativethatalsoantagonizesmGluR5receptors.ItdemonstratesIC50valuesof4.1nMand147nMformGluR1andmGluR5,respectively1.A-794278bindstoaputativeallostericrecognitionsitelocatedwithintheseven-transmembranedomainofthereceptor1,2.
Glutamateisthemostabundantexcitatoryneurotransmitterinthecentralnervoussystem.Itmodulatestheactivityofmanytypesofsynapsesbyactivatinginpartmetabotropicglutamatereceptors(mGluRs).mGluRsconsistofthreegroups:I,II,andIIIwithatotalofeightsubtypes,mGluR1tomGluR8.mGluR1playsanimportantroleinthecentralsensitizationofpainandinavarietyoffunctionswithpotentialimplicationsinneurologicalandpsychiatricdisorders1,2.
A-794278(#A-435) isahighlypure,synthetic,andbiologicallyactivecompound.



