Inhibition of human N-type voltage-gated Ca2+ channels by the neuroprotective agent BW619C89.
Human N-type Ca2+ channels were rapidly and reversibly inhibited by 5-100 microM BW619C89 (IC50 = 16.4 microM at Vtest = + 10 mV and Vhold = - 90 mV). In the presence of 20 microM BW619C89, activation kinetics were significantly faster. The degree of inhibition observed was affected by both test and holding potential, indicating state-dependent interactions with the N-type Ca2+ channel.
McNaughton
N C
NC
Neurobiology Division, MRC Laboratory of Molecular Biology, Cambridge, UK.
Leach
M J
MJ
Hainsworth
A H
AH
Randall
A D
AD
D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002460:Cell Line; D004594:Electrophysiology; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects*; D007700:Kinetics; D018696:Neuroprotective Agents / Q000494:pharmacology*; D010879:Piperazines / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology*; D026941:Sodium Channel Blockers; D015222:Sodium Channels / Q000378:metabolism
D002121:Calcium Channel Blockers; D018696:Neuroprotective Agents; D010879:Piperazines; D011743:Pyrimidines; D026941:Sodium Channel Blockers; D015222:Sodium Channels; C081980:sipatrigine