Metabolism in vitro of radioiodinated N-isopropyl-p-iodoamphetamine by isolated hepatocytes.
An in vitro technique for the determination of radiopharmaceutical metabolism has been developed using isolated hepatocytes. Radioiodinated N-isopropyl-p-iodoamphetamine (IMP; iofetamine, USP) was employed a model tracer in these studies because its labeled metabolites are well-characterized. Hepatocytes isolated from the rat and human produced labeled metabolites in vitro for up to 4 h in a manner similar to that reported for humans in vivo. Identical metabolites were generated by all cell types investigated, but the rate of metabolism differed (rat >> human; female > male; fresh > frozen). The utility of this methodology for the preclinical evaluation of potential radiopharmaceuticals is described.
Moerlein
S M
SM
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110.
Weisman
R A
RA
Beck
D
D
Li
A P
AP
Welch
M J
MJ
D000328:Adult; D000662:Amphetamines / Q000378:metabolism*; D000818:Animals; D015925:Cryopreservation; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes / Q000378:metabolism*; D020367:Iofetamine; D008099:Liver / Q000166:cytology / Q000378:metabolism*; D008297:Male; D051381:Rats; D011916:Rats, Inbred F344; D012737:Sex Factors; D012997:Solvents
D000662:Amphetamines; D007457:Iodine Radioisotopes; D012997:Solvents; D020367:Iofetamine