Abstract：
:T-type Ca(2+) currents were recorded in 2 mM Ca(2+) from HEK293 cells stably expressing the low voltage-activated Ca(2+) channel sub-unit alpha(1I). These currents were inhibited by the known Ca(2+) channel antagonist mibefradil with an IC(50) close to 1 microM. SB-209712 (1,6,bis¿1-[4-(3-phenylpropyl)piperidinyl]¿hexane), a compound originally developed as a high voltage-activated Ca(2+) channel blocker, proved to be a more potent T-type channel antagonist, exhibiting an IC(50) in the region of 500 nM. The antagonism produced by SB-209712 was reversed following drug removal and the observed antagonism exhibited little or no voltage-dependence with respect to either holding or test potential. These data indicate that SB-209712 is amongst the most potent known non-peptide T-type channel antagonists and thus may have some use in understanding the role of these channels in cellular function.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
McNaughton NC,Warre R,Cooper DG,Nasir S,Ranson JL,Randall Adoi
10.1016/s0014-2999(00)00740-8keywords:
subject
Has Abstractpub_date
2000-10-27 00:00:00pages
53-60issue
1-2eissn
0014-2999issn
1879-0712pii
S0014-2999(00)00740-8journal_volume
407pub_type
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