Chemical Name:N,N,N,-Trimethyl-5-[(tricyclo[3.3.1.13,7]dec-1-ylmethyl
)amino]-1-pentanaminiumbromide hydrobromide
Biological Activity:
Voltage-dependent
open-channel blocker of AMPA receptors. Displays selectivity between subtypes,
blocking GluR2 subunit-lacking (Ca2+-permeable) receptors more
potently than GluR2-containing receptors (IC50 values are 2.6 and
1102 μM respectively). Also blocks NMDA receptor-mediated
currents. Anticonvulsant in vivo.
Magazaniket al (1997) Block of open
channels of recombinant AMPA receptors and native AMPA/kainate receptors by
adamantane derivatives. J.Physiol. 505 655. Buldakovaet
al (1999) Characterization of AMPA receptor populations in rat brain cells
by the use of subunit-specific open channel blocking drug, IEM-1460. Brain Res.
846 52. Schlesingeret al (2005) Two mechanisms of
action of the adamantane derivative IEM-1460 at human AMPA-type glutamate
receptors. Br.J.Pharmacol. 145 656.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.