Add time:08/19/2019         Source:sciencedirect.com

The binding sites for papaverine in human intestine were studied with the radioiodinated papaverine derivative, 6,7-dimethoxy-4-(4′-amino,3′-[125I]iodobenzyl)isoquinoline ([125I]DMABI) as a probe. This drug was shown to bind to two specific binding sites in human colon membranes; one with a low capacity (Kd = 0.02 ± 0.01 μM, Bmax = 0.77 ± 0.15 fmol/mg and another with a high capacity (Kd = 12 ± 1.5 μM, Bmax = 167 ± 20 fmol/mg). The ability of various 4-benzyl isoquinolines derivatives, to inhibit radioligand binding was not influenced by 4′-substitutions, but was influenced by 6,7-substitutions, e.g. 6-hydroxy > 7-hydroxy > 6,7-dihydroxy; and by other substitutions, e.g. 1-CH3 > N-oxyde. The papaverine probe was further used to examine structural aspects of human colon papaverine binding sites. For this purpose, [125I]DMABI-labeled membranes were irradiated with U.V. for 15 min at 4°C. Subsequent sodium dodecyl sulfate-polyacrylamide gel electrophoresis of membranes revealed a major, specifically labeled protein of Mr = 36 000 Da. This photoaffinity labeling was protected by unlabeled DMABI in a dose-dependent manner (IC50: 0.5 μM).

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