The enzyme-inhibitor approach to cell-selective labelling--II. In vivo studies with pIBS in small animals and man.
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).
Singh
J
J
Department of Chemistry, University of Southampton, England.
Wyeth
P
P
Ackery
D M
DM
Zivanovic
M A
MA
D000818:Animals; D001682:Biological Availability; D002257:Carbonic Anhydrase Inhibitors / Q000493:pharmacokinetics* / Q000633:toxicity; D004337:Drug Carriers; D004912:Erythrocytes / Q000378:metabolism; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D008297:Male; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D013449:Sulfonamides / Q000493:pharmacokinetics* / Q000633:toxicity; D014018:Tissue Distribution; D000096926:Benzenesulfonamides
D002257:Carbonic Anhydrase Inhibitors; D004337:Drug Carriers; D007457:Iodine Radioisotopes; D013449:Sulfonamides; C069442:4-iodobenzenesulfonamide; D000096926:Benzenesulfonamides