title: (125)I labeling of clomiphene and biodistribution studies for possible use as a model in breast cancer imaging.
abstract: Clomiphene has growth-inhibitory effects of breast cancer cells, clomiphene was successfully labeled with (125)I via direct electrophilic substitution reaction with labeling yield 97%. It was obtained at optimum substrate amount of 0.5mg, Chloramine-T was used as an oxidizing agent at optimum amount of 25µg. Labeling reactions was done at pH 5 at ambient temperature. This study showed good in vitro and in vivo stability of the (125)I-clomiphene. The radiolabeled compound showed high ascetic fluid uptake of 18.12±0.27% at 30min post-injection. Solid tumor uptake of (125)I-clomiphene was 12.48±0.32% at 30min post-injection. This data revealed the localization of tracer in tumor tissue with high percent sufficient to use (125)I-clomiphene as a promising tool for the diagnosis of breast cancer.
authors.affiliation: Labeled Compound Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo 11371, Egypt; Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: I T
authors.initials: IT
authors.lastname: Ibrahim
authors.affiliation: Labeled Compound Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo 11371, Egypt; Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: M T
authors.initials: MT
authors.lastname: El-Kolaly
authors.affiliation: Labeled Compound Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo 11371, Egypt; Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: M H
authors.initials: MH
authors.lastname: Aboumanei
authors.affiliation: Labeled Compound Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo 11371, Egypt; Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: A
authors.initials: A
authors.lastname: Abdelbary
mesh_terms: D001943:Breast Neoplasms / Q000000981:diagnostic imaging*; D045744:Cell Line, Tumor; D002700:Chloramines; D002996:Clomiphene / Q000493:pharmacokinetics*; D004965:Estrogen Antagonists / Q000493:pharmacokinetics*; D006801:Humans; D007553:Isotope Labeling; D014018:Tissue Distribution; D014105:Tosyl Compounds
chemical_list: D002700:Chloramines; D004965:Estrogen Antagonists; D014105:Tosyl Compounds; C016300:chloramine-T; D002996:Clomiphene
keywords: (125)I-clomiphene; Antiestrogen; Biodistribution; Labeling; Solid tumor