Overview
- Hupe, D.J. et al. (1991) J. Biol. Chem. 266, 10136.
- Guo, L. et al. (1991) Eur. J. Pharmacol. 538, 15.
Alomone Labs L-651,582 blocks L-type Ca2+ currents in Xenopus oocytes.A. Time course of L-type channel (CaV1.2+α2δ1+β1a) activity before and during applications of 1, 10 and 100 μM L-651,582 (#L-110) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to 0 mV. Periods of compound application are indicated by symbols in the inset. B. Example of superimposed current traces before and during application of 1, 10 and 100 μM L-651,582 (taken from the experiment described in A).
Two subtypes of voltage-gated Ca2+ channels (VGCC, CaV) are found in most non-excitable cells, the T-type (CaV3) and the L-Type (CaV1) Ca2+ channels1-2.
L-651,582 is an anti-proliferative, anti-angiogenic, anti-metastatic and anti-parasitic agent3-5, which is also selective towards numerous mismatch repair-deficient tumor cell lines in vitro.6 It is a voltage-gated L-type Ca2+ channel blocker with an IC50 of 0.5 µg/ml5 . Patch clamp measurements of current through L- and T-type channels in guinea pig atrial cells also indicate that L-651,582 is a Ca2+ antagonist5. Block of L-type Ca2+ channels is voltage-dependent and the apparent dissociation constant for the high affinity state is 0.2 µg/ml. The IC50 for block of T-type Ca2+ channels is 1.4 µg/ml5.
