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OurBioassay
- Allan,R.D. etal. (1990) J.Med.Chem. 33, 2905.
- Erreger,K. etal. (2007) Mol.Pharmacol. 72, 907.
- AlomoneLabstrans-ACBDactivatesNMDAreceptors(NR1+NR2A)expressedinXenopusoocytes.TimecourseofNMDAreceptorcurrentactivationby2and10μM trans-ACBD (#A-280)(at-80mV).Forcomparison,asolutioncontaining10µMglutamateand10µMglycinewasappliedfor2.5minresultingincurrentsofcomparableamplitude(asindicated).Amplitudechangeasaresultoftheapplicationofraisingconcentrationsoftrans-ACBD(perfusiondurationindicatedbythehorizontalbar,concentrationasindicated).
- 1.Fletcher,E.J. etal. (1991) Neurosci.Lett. 121, 133.
- 2.Allan,R.D. etal. (1990) J.Med.Chem. 33, 2905.
- 3.Talukder, I. etal.(2010) J.Neurosci. 30, 11792.
trans-ACBDisapotent,competitiveandselectiveactivatorofglutamateuptake.ThecompoundactsasanNMDA(N-methyl-D-aspartate)receptoragonist.TheACBDstructureincludestwoisomers:cis-1-aminocyclobutane-1,3-dicarboxylicacidandtrans-1-aminocyclobutane-1,3-dicarboxylicacid.Severalstudieshaveshownthatthetransisomerismorepotentthanthecisisomer.Thetransisomerwasalsoshowntobe20timesmoreactivethanNMDA1,2,themajorexcitatoryneurotransmitterinthemammaliancentralnervoussystem(CNS).
SeveralstudiessuggestthatmodificationsandchangesofglutamateuptakecouldplayaroleinprocessesunderlyingsynapticplasticityintheCNS2.
NMDAreceptorsareionchannelsgatedbyglutamate.Glutamate-mediatedsignalingisimportantforbasicneuron-neuronsignalingandneuronalprocessessuchaslearning,memoryandpainperception3.
trans-ACBD(#A-280) isahighlypure,synthetic,andbiologicallyactivecompound.