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. 2022 Jan;101(1):56–67. doi: 10.1124/molpharm.121.000349

TABLE 1.

Potencies of mibefradil and ML218 to inhibit calcium influx produced by PROG, PGE1, l-sirenin, and high K+/high pH in human sperm

Opener Blocker pIC50 n
PROG mibefradil 5.17 ± 0.24 7
ML218 5.02 ± 0.08 4
PGE1 mibefradil 5.08 ± 0.31 8
ML218 4.87 ± 0.15 3
l-sirenin mibefradil 5.09 ± 0.34 5
ML218 4.85 ± 0.17 3
high K+/high pH mibefradil 4.76 ± 0.09 8
ML218 4.99 ± 0.16 7

Inhibitors were evaluated in the presence of an EC80 concentration of each activator (30 nM PROG, 10 nM PGE1, 3 µM l-sirenin). Buffer containing 140 mM K+, pH 8.2 was added to elicit alkalinization/depolarization calcium influx. pIC50 values are expressed as the mean ±SD with the number of independent experiments indicated by n.