The NMDA receptor antagonist eliprodil (SL 82.0715) blocks voltage-operated Ca2+ channels in rat cultured cortical neurons.
The effect of the non-competitive NMDA receptor antagonist eliprodil on NMDA receptor- and voltage-operated Ca2+ currents was investigated in rat cultured cortical neurons by using the whole-cell patch clamp technique. With neurons voltage-clamped at -40 mV, eliprodil reduced in a concentration-dependent manner the inward current induced by N-methyl-D-aspartate (NMDA) (10 microM) in the presence of D-serine with an IC50 of 0.67 microM (Imax = 83%). Eliprodil also blocked the total inward Ba2+ current carried in part by L- and N-type Ca2+ channels with an IC50 of 1.48 microM (Imax = 87%). These results suggest that the neuroprotective properties of eliprodil could be due to its combined ability to antagonize the NMDA receptor- and voltage-operated Ca2+ channels.
Biton
B
B
Synthélabo Recherche, Preclinical Research Department, Bagneux, France.
Granger
P
P
Carreau
A
A
Depoortere
H
H
Scatton
B
B
Avenet
P
P
D000818:Animals; D015220:Calcium Channels / Q000187:drug effects*; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D004594:Electrophysiology; D009474:Neurons / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
D015220:Calcium Channels; D010880:Piperidines; D016194:Receptors, N-Methyl-D-Aspartate; C058083:eliprodil