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- MABIre,D. etal.(2005) J.Med.Chem. 48, 2134.
- Lavreysen,H. etal.(2003) Mol.Pharmacol. 63, 1082.
- VanWagenen,B.C. etal. (2000) Abstr.Soc.Neurosci. PresentationNo. 618, 3.
AlomoneLabsNPS2390inhibitsmGluR1-mediatedCa2+ mobilizationinU2OScells.DoseresponseofnormalizedinhibitionofhumanmGluR1mediated,L-GlutamateevokedCa2+ mobilizationby NPS2390 (#N-340).IC50 wasdeterminedat56.7nM.hmGluR1-expressingcellswereloadedwithcalcium-sensitivedye,incubatedwitharangeofconcentrationsofNPS2390,andstimulatedby15µML-Glutamate(EC80).ChangesinintracellularCa2+ followingstimulationweredetectedaschangesinmaximumrelativefluorescence(RLU)usingFLIPRTETRA™.
- 1.Mabire,D. etal.(2005) J.Med.Chem. 48, 2134.
- 2.Lavreysen,H. etal.(2003) Mol.Pharmacol. 63, 1082.
- 3.VanWagenen,B.C. etal. (2000) Abstr.Soc.Neurosci. PresentationNo. 618, 3.
- 4.O"Brien,J.A. etal. (2003) Mol.Pharmacol. 64, 731.
- 5.Satow,A. etal. (2008) J.Pharmacol.Exp.Ther. 326, 577.
- 6.Eom,H.S. etal. (2016) PLoSOne 11, e0147538.
- 7.Lu,Y.M. etal. (1996) J.Neurosci. 17, 5196.
NPS2390,aquinoxalinederivative,isasynthetic,potent,selectiveandnon-competitiveantagonistofgroupImetabotropicglutamatereceptorscomprisingmGluR1andmGluR5receptorswithIC50valuesof5.2and8.2nMrespectively7.ThecompoundshowsverylowaffinitytowardsothermGluRreceptors.
SeveralstudiessuggestthatNPS2390actsonasitethatisdifferentfromtheglutamatebindingpocket.ItislikelythatthecompoundactsatthetransmembranesegmentVIIregionofthereceptors1-3.
Metabotropicglutamatereceptors(mGluRs)areGproteincoupledreceptors(GPCR)thatplayanimportantroleinsynapticplasticityandotherneuro-physiologicalandpathologicalprocessesincludingamajorroleincentralsensitizationandneuropathicpain.Type1mGluRsaremainlyfoundinsomatodendriticdomainsandpostsynapticallyregulateneuronalexcitabilityandsynaptictransmissionthroughseveralintracellularsecondmessengersystems4,5.ThemGlu1receptorsplayanimportantroleinmotorlearningandmotorcoordinationwhereasmGlu5receptorscontributetoinductionoflong-termpotentiationandassociativelearning6.
NPS2390(#N-340) isahighlypure,synthetic,andbiologicallyactivecompound.



