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- Allan,R.D.etal.(1990)J.Med.Chem. 33,2905.
- Erreger,K.etal.(2007)Mol.Pharmacol.72,907.
AlomoneLabscis-ACBDactivatesNMDAreceptors(NR1+NR2A)expressedinXenopusoocytes.TimecourseofNMDAreceptorcurrentactivationby1to500μM cis-ACBD (#A-281)(at-80mV).Amplitudechangeasaresultoftheapplicationofrisingconcentrationsofcis-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-dicarboxylicacidand trans-1-aminocyclobutane-1,3-dicarboxylicacid.Severalstudieshaveshownthatthe trans isomerismorepotentthanthe cis isomer.The trans isomerwasalsoshowntobe20timesmoreactivethan NMDA1,2,themajorexcitatoryneurotransmitterinthemammaliancentralnervoussystem(CNS).
SeveralstudiessuggestthatmodificationsandchangesofglutamateuptakecouldplayaroleinprocessesunderlyingsynapticplasticityintheCNS2.
NMDAreceptorsareionchannelsgatedbyglutamate.Glutamate-mediatedsignalingisimportantforbasicneuron-neuronsignalingandneuronalprocessessuchaslearning,memoryandpainperception3.
cis-ACBD(#A-281) isahighlypure,synthetic,andbiologicallyactivecompound.



