title: Clinical evaluation of 99mTc diaminocyclohexane, a renal tubular agent with cationic transport: results in healthy human volunteers.
abstract: As alternatives to anionically transported hippuran, structure distribution experiments on a series of 99mTc-labelled primary substituted ethylene diamine compounds led to selection of 99mTc diaminocyclohexane (DACH) for clinical evaluation, 99mTc DACH, a cation with the structure trans-[O2(DACH)2 99mTc]+ is prepared by mixing 50 mumol DACH, 1 mumol stannous tartrate and 500 MBq of 99mTc. Seven normal volunteers underwent renal imaging and clearance studies using 150 MBq of 99mTc DACH and 1 MBq of 125I hippuran simultaneously. The images with 99mTc DACH revealed good uptake and excretion. The mean +/- 2 SD values of parenchymal and whole-kidney transit time indices and mean parenchymal transit time were 46 +/- 33, 75 +/- 64 and 141 +/- 51 s, respectively, similar to mercaptoacetyl triglycine. The mean clearance of 99mTc DACH was found to be 163 ml/min (SD = 32). Following cationic blockade with 900 mg oral thiamine, significant reduction (p < 0.001) in DACH clearance was noted, but hippuran clearance remained unaltered. The results support the hypothesis that 99mTc DACH is transported cationically.
authors.affiliation: Department of Nuclear Medicine, St. Bartholomew's Hospital, London, UK.
authors.forename: A K
authors.initials: AK
authors.lastname: Padhy
authors.forename: K K
authors.initials: KK
authors.lastname: Solanki
authors.forename: J
authors.initials: J
authors.lastname: Bomanji
authors.forename: T
authors.initials: T
authors.lastname: Chaiwatanarat
authors.forename: C C
authors.initials: CC
authors.lastname: Nimmon
authors.forename: K E
authors.initials: KE
authors.lastname: Britton
mesh_terms: D000328:Adult; D001692:Biological Transport / Q000187:drug effects; D002412:Cations / Q000493:pharmacokinetics; D003514:Cyclohexylamines; D005919:Glomerular Filtration Rate; D006801:Humans; D007465:Iodohippuric Acid / Q000493:pharmacokinetics; D007668:Kidney / Q000000981:diagnostic imaging / Q000378:metabolism; D007684:Kidney Tubules / Q000000981:diagnostic imaging* / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics* / Q000652:urine; D011877:Radionuclide Imaging; D013831:Thiamine / Q000494:pharmacology
chemical_list: D002412:Cations; D003514:Cyclohexylamines; D015609:Organotechnetium Compounds; C084614:technetium Tc 99m diaminocyclohexane; D007465:Iodohippuric Acid; D013831:Thiamine