In vitro activity: Eliprodil (formerly known as SL-820715) is a non-competitive NR2B-NMDA receptor antagonist with IC50 value of 1 uM, it is less potent for NR2A- and NR2C-containing receptors with IC50> 100 uM. NMDA receptors play a key role in mediating glutamate-induced excitotoxicity, thus it is believed that NMDA antagonists would be neuroprotective after a stroke or other traumatic brain injury. Eliprodil protects pyramidal neurons in hippocampal slices from hypoxic or ischemic damage. Eliprodil also stimulates CNS myelination and may have potential for multiple sclerosis.

Kinase Assay: NR2B-NMDA antagonist Human N-type Ca2+ channel currents were inhibited by ifenprodil and eliprodil with IC50 values of 50 microM and 10 microM respectively whereas P-type Ca2+ channel currents were inhibited reversibly by ifenprodil and eliprodil with approximate IC50 values of 60 microM and 9 microM respectively. eliprodil (1 microm) produced a moderate reverse rate-dependent prolongation of the action potential duration (7.4+/-1.5, 8.9+/-2.1 and 9.9+/-1.8% at cycle lengths of 300, 1000 and 5000 ms, respectively; n=9).

Cell Assay: Recombinantly expressed human alpha 1B-1 alpha 2b beta 1-3 Ca2+ subunits in HEK293 cells, which results in an omega-conotoxin-sensitive neuronal N-type voltage-dependent Ca2+ channel and omega-Aga IVA sensitive Ca2+ channels (P-type) in acutely isolated cerebellar Purkinje neurones were reversibly inhibited by ifenprodil and eliprodil.