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. Author manuscript; available in PMC: 2013 Nov 15.
Published in final edited form as: Bioorg Med Chem. 2012 Sep 25;20(22):6613–6620. doi: 10.1016/j.bmc.2012.09.022

Table 1.

IDHP activity at VGCC and MDR-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.