Affinities of different DHPs for brain membranes of Cav1.2DHP(−/−) and wild-type mice
Ligand concentration was 0.14-0.18 nM. Membrane protein concentration was 0.3 mg/ml. Data are given as means ± S.D. for the indicated number of experiments. Statistical significance of selectivity was determined from a direct comparison of IC50 values and from the selectivity ratios (WT:MUT) calculated from individual experiments carried out in parallel for both genotypes.
Dihydropyridine | WT | Cav1.2DHP(−/−) | IC50 WT:MUT | n |
|---|---|---|---|---|
| (±)-Isradipine | ||||
| IC50 (nM) | 0.43 ± 0.03 | 0.59 ± 0.12 | 0.76 ± 0.20 | 3 |
| Slope factor | 0.99 ± 0.10 | 0.98 ± 0.08 | ||
| Azidopine | ||||
| IC50 (nM) | 1.23 ± 0.71 | 1.08 ± 0.56 | 1.13 ± 0.18 | 3 |
| Slope factor | 0.94 ± 0.04 | 0.95 ± 0.04 | ||
| Nitrendipine | ||||
| IC50 (nM) | 0.97 ± 0.11 | 2.79 ± 0.80+++ | 0.37 ± 0.11** | 4 |
| Slope factor | 0.89 ± 0.08 | 0.96 ± 0.10 | ||
| Nifedipine | ||||
| IC50 (nM) | 3.42 ± 0.55 | 13.21 ± 1.05+++ | 0.26 ± 0.06** | 3 |
| Slope factor | 0.85 ± 0.04 | 0.87 ± 0.11 | ||
| (−)-Isradipine | ||||
| IC50 (nM) | 35.2 ± 7.4 | 35.5 ± 5.2 | 0.98 ± 0.09 | 3 |
| Slope factor | 0.95 ± 0.01 | 0.86 ± 0.07 | ||
| Amlodipine | ||||
| IC50 (nM) | 41.1 ± 1.2 | 39.2 ± 4.6 | 1.06 ± 0.14 | 3 |
| Slope factor | 0.93 ± 0.04 | 1.01 ± 0.02 |
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