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The enzyme-inhibitor approach to cell-selective labelling—II. In vivo studies with pIBS in small animals and man

✍ Scribed by Jaspal Singh; Paul Wyeth; Duncan M. Ackery; Maureen A. Zivanovic

Publisher: Elsevier Science
Year: 1991
Weight: 695 KB
Volume: 42
Category: Article
ISSN: 0883-2889
DOI: 10.1016/0883-2889(91)90086-g

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✦ Synopsis

p-Iodobenzenesulphonamide (pIBS), a potent red cell carbonic anhydrase inhibitor, was used as a carrier for radioiodine in the enzyme-inhibitor approach to cell-specific blood labelling. Radioactivity distribution was monitored in rats and man following i.v. administration of the radiolabelled carrier or of pre-labelled red cells. Rat blood activity fitted a two compartment model; the half-life for overall elimination was 69 +/- 27 h. At 24 h most activity remained associated with red cells, but there was a significant uptake in the large intestine (10 +/- 6%). In man there was no significant accretion by gut or any other organ over 93 h, and the blood clearance was mono-exponential (t1/2 = 9.8 +/- 1.5 days).

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The enzyme-inhibitor approach to cell-selective labelling—I. Sulphonamide inhibitors of carbonic anhydrase as carriers for red cell labelling: in vitro uptake of pIBS by human red blood cells

✍ Jaspal Singh; Paul Wyeth 📂 Article 📅 1991 🏛 Elsevier Science ⚖ 925 KB

Red cell carbonic anhydrase is identified as an ideal target in an enzyme-inhibitor approach to radiolabel localisation. Current problems in blood pool labelling could be overcome by using selective sulphonamide inhibitors as carriers. p-Iodobenzenesulphonamide (pIBS) was selected as the choice reag