title: Influence of pretreatment with 3-amino-1-hydroxypropylidene-1,1-bisphosphonate (APB) on organ uptake of 211At and 125I-labeled amidobisphosphonates in mice.
abstract: To minimize nontarget organ uptake in animals receiving radiolabeled amidobisphosphonates, the influence of pretreatment with cold 3-amino-1-hydroxypropylidene-1,1-bisphosphonate (APB, pamidronate) was studied. Three groups of animals were given pure 3-[125I]iodobenzamide-N-3-hydroxypropylidene-3,3-bisphosphonate (IBPB) and 3-[211At]astatobenzamide-N-3-hydroxypropylidene-3,3-bisphosphonate (ABPB) (control); co-injection of APB and IBPB/ABPB; and 1 h preinjection of APB followed by IBPB/ABPB, respectively. A significant reduction of uptake in normal tissue was observed, whereas the bone uptake remained constant at 35-50%ID/g tissue. This study suggests that co- or preinjection of pamidronate may reduce the normal organ radiation doses when using these radiohalogenated bisphosphonates for endoradiotherapeutic procedures.
authors.affiliation: Department of Chemistry, University of Oslo, Norway.
authors.forename: K M
authors.initials: KM
authors.lastname: Murud
authors.forename: R H
authors.initials: RH
authors.lastname: Larsen
authors.forename: O S
authors.initials: OS
authors.lastname: Bruland
authors.forename: P
authors.initials: P
authors.lastname: Hoff
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001246:Astatine / Q000737:chemistry; D001842:Bone and Bones / Q000378:metabolism; D004164:Diphosphonates / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology*; D005269:Femur / Q000378:metabolism; D007457:Iodine Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009928:Organ Specificity; D000077268:Pamidronate; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: C403881:3-astatobenzamido-N-3-hydroxypropylidene-3,3-bisphosphonate; C403880:3-iodobenzamido-N-3-hydroxypropylidene-3,3-bisphosphonate; D000970:Antineoplastic Agents; D004164:Diphosphonates; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D000077268:Pamidronate; D001246:Astatine