Add time:08/18/2019         Source:sciencedirect.com

In rat tissues, the specific binding of 6,7-dimethoxy 4-(4'-amino, 3'(125I)iodobenzyl)-isoquinoline is distributed as follows: aorta > pancreas > liver > intestine > stomach > lung > skeletal muscle > heart > brain. In aorta and intestine 125I-DMABI is specifically covalently incorporated after direct u.v. photolabeling, in a major polypeptide of Mr 36,000 daltons, and a minor polypeptide of Mr 52,000 daltons. In intestine another smaller minor polypeptide of Mr 26,000 is observed. In intestine a variety of isoquinolines are tested for their ability to inhibit the covalent photo-incorporation of 125I-DMABI. Inhibitory potency is influenced by 6,7-substitutions, e.g. 6,7-dimethoxy, and by the presence of benzyl ring in C-1 and C-4 positions. Isoquinoline is much more potent than tetrahydroisoquinoline. 125I-DMABI intestinal bincling site is solubilized using Triton X-100. Layered on Sephadex G-25 column, a high specific peak of radioactivity is eluted in the void volume of the column. The 125I-DMABI bincling protein loaded onto a Sephacryl S-300 column is eluted as a single peak corresponcling to a species with a Stokes radius of 43.5 Å. The sedimentation coefficient of the 125I-DMABI bincling protein is measured by ultracentifugation of 5.5 S, using 5–20% sucrose gradient. The calculated molecular weight of the intestinal 125I-DMABI bincling protein is estimated at 110,000 daltons.

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