title: BMS181321 accumulation in rodent and human cells: the role of P-glycoprotein.
abstract: A 2-nitroimidazole with a side chain that contains technetium-99m as a chelate, BMS181321, is undergoing evaluation as an imaging agent for myocardial and cerebral ischaemia, as well as a diagnostic probe for hypoxic cells in solid tumours. Its accumulation in hypoxic and aerobic populations of three lines of Chinese hamster ovary cells of differing P-glycoprotein status, as well as one rat and two human cell lines has been determined. There was selective accumulation of BMS181321 in hypoxic vs aerobic cells. P-glycoprotein level was not a factor in this accumulation and hypoxic human cells accumulated BMS181321 more rapidly than the rodent cells. These results indicate P-glycoprotein levels in tumour cells will not confound the use of BMS181321 as a hypoxic cell marker.
authors.affiliation: Department of Medical Biophysics, University of Toronto, Canada.
authors.forename: D S
authors.initials: DS
authors.lastname: Cowan
authors.forename: T
authors.initials: T
authors.lastname: Melo
authors.forename: L
authors.initials: L
authors.lastname: Park
authors.forename: J R
authors.initials: JR
authors.lastname: Ballinger
authors.forename: A M
authors.initials: AM
authors.lastname: Rauth
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000032:analysis / Q000502:physiology*; D000818:Animals; D016466:CHO Cells; D015687:Cell Hypoxia; D006224:Cricetinae; D004351:Drug Resistance; D006801:Humans; D009369:Neoplasms / Q000378:metabolism; D009593:Nitroimidazoles / Q000493:pharmacokinetics*; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D051381:Rats
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D009593:Nitroimidazoles; D015609:Organotechnetium Compounds; C082027:BMS 181321