Non-competitive NMDA receptor antagonist (IC50 = 1.25 μM). Binds to ion channel site.
Shows low affinity but has rapid blocking and unblocking ability at the NMDAR.
Selectively blocks extrasynaptic NMDARs.
Enhances hippocampal long-term potentiation (LTP) and reverses LTP suppression.
Improves cognitive function and shows anti-Alzheimer's activity.
The voltage sensitive NMDA receptor antagonist memantine is effective at concentrations of 10-100 µM. In CA1 hippocampal neurons held at – 30 Mv, Hello Bio memantine (at 100 µM) gradually inhibited evoked NMDA receptor mediated excitatory currents over time (see Fig 1 above).
#Protocol 1: Assay evoked NMDAR currents at -30 mV (used for memantine)
NMDAR currents were recorded via whole cell voltage clamp recordings of CA1 pyramidal neurons from the rat hippocampal brain slice and evoked via a stimulating electrode placed in the CA3 region to stimulate the Schaffer collateral pathway.
Each NMDAR current was evoked via a single square (150 µs) pulse every 10 sec at a stimulus intensity that gave a reliable NMDAR current.
Neurons were constantly held at -30 mV and NMDAR currents recorded in response to continual bath applications of NMDAR antagonists.
All NMDAR recordings were made in the presence of GABAA-R and AMPA-R antagonists.
Solubility & Handling
Soluble in water (100mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
The N-methyl-D-aspartate receptor channel blockers memantine, MRZ 2/579 and other amino-alkyl-cyclohexanes antagonise 5-HT(3) receptor currents in cultured HEK-293 and N1E-115 cell systems in a non-competitive manner.
Rammes G et al (2001) Neurosci Lett 306(1-2) : 81-4.