Synthesis of dendrimer-based biotin radiopharmaceuticals to enhance whole-body clearance. Academic Article uri icon

Overview

abstract

  • To synthesize a biotin radiopharmaceutical that clears rapidly, dendrimer was used as a carrier and conjugated with succinimidyl 3-[(125)I]iodobenzoate and tetrafluorophenyl norbiotinamidosuccinate. Then, succinic anhydride was used to reduce its pI. In mice, the non-succinylated product showed high liver (67% ID/g) and kidney (44% ID/g) uptakes and whole-body retention (94% ID) at 20 min that persisted for 12 hr. The corresponding organ uptakes (22% and 11% ID/g) and the whole-body retention (47% ID) were drastically reduced by succinylation (p<0.0001). Lysine co-injection further lowered renal uptake.

publication date

  • August 1, 2003

Research

keywords

  • Amines
  • Biotin
  • Iodobenzoates
  • Isotope Labeling
  • Kidney
  • Liver

Identity

Scopus Document Identifier

  • 0142106850

Digital Object Identifier (DOI)

  • 10.1016/s0969-8051(03)00052-0

PubMed ID

  • 12900287

Additional Document Info

volume

  • 30

issue

  • 6