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Vol. 54, Issue 6, 1080-1087, December 1998
Department of Neurobiology, Harvard Medical School, Boston,
Massachusetts 02115
The antihypertensive agent mibefradil completely and reversibly
inhibited T-type calcium channels in freshly isolated rat cerebellar
Purkinje neurons. The potency of mibefradil was increased at less
hyperpolarized holding potentials, and the apparent affinity was
correlated with the degree of channel inactivation. At 35°, the
apparent dissociation constant Kapp was 1 µM at a holding voltage of 
110 mV (corresponding to
noninactivated channels) and 83 nM at a holding voltage of
70 mV (corresponding to 65% inactivation). The increased affinity
was attributable mainly to a decreased off-rate. Mibefradil also
inhibited P-type calcium channels in Purkinje neurons, but inhibition
was much less potent. At a holding potential of 70 mV, the
Kapp for mibefradil inhibition of P-type
channels was ~200-fold higher than that for inhibition of T-type
channels. Mibefradil should be a useful compound for distinguishing
T-type channels from high voltage-activated calcium channels in neurons
studied in vitro.
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