Table 1.
IDHP | R1 | R2 | VGCC Ki (nM) | VGCC Patch Clamp (M) | Ref. | MDR-1 (% inh.) |
---|---|---|---|---|---|---|
1a | CH3 | C6H5 | 13.9 | 12,13,15 | 48.9 | |
1b | CH3 | o-MeO-C6H4 | 17.1 | 19 | 32.8 | |
1c | CH3 | 2-MeO-5-Cl-C6H3 | 6.86 | 19 | 15.0 | |
1d | CH3 | o-Cl-C6H4 | 9.68 | 19 | 10.9 | |
1e | CH3 | m-Cl-C6H4 | 1.98 | 19 | 26.8 | |
1f | CH3 | p-Cl-C6H4 | 1.31 | 19 | 11.7 | |
1g | i-Pr | C6H5 | a | 14 | 38.4 | |
1h | C6H5CH2CH2 | C6H5 | 55.3 | 18 | 27.6 | |
1i | p-Biphenyl-CH2CH2 | CH3 | 8.69 | 18 | 18.6 | |
1j | 1-naphthyl CH2CH2 | CH3 | 4.1 | 0.47 | 18,19 | 19.0 |
1k | m-Br-C6H5CH2(CH3)CH | CH3 | this work | 61.2 | ||
1l | 1-naphthyl CH2(CH3)CH | CH3 | this work | 38.3 |
a weak vasodilator in the Langendorff perfused heart assay.