title: Synthesis and in vivo biodistribution of BPA-Gd-DTPA complex as a potential MRI contrast carrier for neutron capture therapy.
abstract: p-boronophenylalanine (BPA) conjugated Gd-DTPA complex (3) was synthesized from the active methyne compound 6, the allylic carbonate 7, and BPA by the palladium-catalyzed allylation reaction followed by the DCC coupling reaction. The in vivo biodistribution of complex 3 was evaluated by prompt gamma-ray analysis and alpha-autoradiography using the tumor-bearing rats. High accumulation of gadolinium was observed in the kidney and the %ID values were 0.17 and 0.088 at 20 and 60 min after injection of 3, respectively. The accumulation was also observed in the tumor and the %ID values were 0.010 and 0.0025 at 20 and 60 min after injection, respectively. The visualization experiment of boron distribution in the tumor-bearing rat by alpha-autoradiography indicates that boron was accumulated in the tumor and the intestines at 20 min after injection.
authors.affiliation: Department of Chemistry, Graduate School of Science, Tohoku University, Sendai 980-8578, Japan.
authors.forename: Kazunori
authors.initials: K
authors.lastname: Takahashi
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Nakamura
authors.forename: Shozo
authors.initials: S
authors.lastname: Furumoto
authors.forename: Kazuyoshi
authors.initials: K
authors.lastname: Yamamoto
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Fukuda
authors.forename: Akira
authors.initials: A
authors.lastname: Matsumura
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Yamamoto
mesh_terms: D000818:Animals; D001345:Autoradiography; D001896:Boron Compounds / Q000737:chemistry* / Q000493:pharmacokinetics*; D016754:Boron Neutron Capture Therapy; D003287:Contrast Media / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D019786:Gadolinium DTPA / Q000737:chemistry / Q000493:pharmacokinetics*; D009682:Magnetic Resonance Spectroscopy; D009374:Neoplasms, Experimental / Q000473:pathology / Q000628:therapy*; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000493:pharmacokinetics*; D051381:Rats; D013055:Spectrophotometry, Infrared; D014018:Tissue Distribution
chemical_list: D001896:Boron Compounds; D003287:Contrast Media; D010649:Phenylalanine; D019786:Gadolinium DTPA; C033685:4-boronophenylalanine