Ifenprodil and eliprodil are both non-competitive NMDA receptor antagonists which have been shown to inhibit neuronal Ca 2+ channel currents. We have examined the effects of these agents on two defined subtypes of voltage-dependent Ca 2+ channels and in the gerbil model of global cerebral ischaemia. Recombinantly expressed human α 1B-1 α 2b β 1–3 Ca 2+ subunits in HEK293 cells, which results in an ω-conotoxin-sensitive neuronal N-type voltage-dependent Ca 2+ channel and ω-Aga IVA sensitive Ca 2+ channels (P-type) in acutely isolated cerebellar Purkinje neurones were reversibly inhibited by ifenprodil and eliprodil. Human N-type Ca 2+ channel currents were inhibited by ifenprodil and eliprodil with IC 50 values of 50 μM and 10 μM respectively whereas P-type Ca 2+ channel currents were inhibited reversibly by ifenprodil and eliprodil with approximate IC 50 values of 60 μM and 9 μM respectively. Maximum current block observed for both channel subtypes was approximately 80% for both ifenprodil and eliprodil. For neuroprotection studies, animals were subjected to 5 min bilateral carotid artery occlusion with or without administration of either ifenprodil or eliprodil (5, 10 or 20 mg/kg i.p.) immediately after surgery followed by two further doses (2.5, 5 or 10 mg/kg, respectively) at 3 and 6 h post-occlusion. Both compounds provided significant protective effects against ischaemia-induced neurodegeneration in the CA1 region of the hippocampus. These results indicate that both ifenprodil and eliprodil protect against ischaemia-induced neurodegeneration when administered post-occlusion and that they also block N and P-type voltage-dependent Ca 2+ channels.
European Journal of Pharmacology – Elsevier
Published: Mar 28, 1996
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