99Tcm-p-aminohippuric acid as a new renal agent.

ABSTRACT

99Tcm-p-aminohippuric acid (99Tcm-PAH) is a new renal radiopharmaceutical prepared from a lyophilized kit by the addition of sodium pertechnetate (Na99TcmO4). Each vial contains PAH, the calcium trisodium salt of diethylenetriamine pentaacetic acid (CaNa3DTPA) and stannous chloride (SnCl2.2H2O) in an inert atmosphere. It is a stable radiopharmaceutical with high radiochemical purity (> 95%). Its protein binding is very similar to that of 131I-OIH, but it is hydrophilic in character. Animal studies using 99Tcm-PAH have indicated that it provides renal images of satisfactory quality with no external background. Despite its almost identical radiochemical purity and HPLC analysis results to 99Tcm-DTPA, 99Tcm-PAH is rapidly secreted by the kidneys in a manner consistent with tubular secretion, as confirmed by rat probenecid studies, whereas 99Tcm-DTPA is excreted by glomerular filtration. The pharmacokinetic parameters of 99Tcm-PAH (t1/2(alpha)) = 2.5 min, t1/2(beta) = 41.7 min, Cl = 5.22 ml.min-1, Kel = 5.1 x 10(-4) min-1) differ from those of 99Tcm-DTPA. Evaluation of 99Tcm-PAH in two human volunteers confirmed its good renal characteristics rapid disappearance from the vascular system, high uptake in kidneys followed by its very fast elimination, and low residual activity 20 min after its intravenous administration.