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Preliminary evaluation of a new radiolabelled biphosphonate
Author(s) -
Larsen Roy H.,
Bruland Øyvind S.
Publication year - 1998
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(1998090)41:9<823::aid-jlcr135>3.0.co;2-q
Subject(s) - chemistry , bisphosphonate , pharmacokinetics , reagent , femur , high performance liquid chromatography , chromatography , medicine , osteoporosis , surgery , organic chemistry
A new bisphosphonate was synthesized using N‐succinimidyl‐3‐[ 125 I]iodobenzoate and 3‐amino‐1‐hydroxypropylidene as the reagents. After purification by reverse phase chromatography the product, 3‐[ 125 I]iodobenzamide‐N‐3‐hydroxypropylidene‐3,3‐bisphosphonate, was injected intravenously into nude mice and the radioactivity content in various normal tissues was measured. Both at 3 h and at 17 h after injection a highly selective bone uptake was observed. Average ratios femur/blood and skull/blood were 35.9 and 36.6 at 3 h and 111.6 and 128.0 at 17 h, respectively. While clearing was observed for all other tissues, the bone radioactivity content did not decrease significantly from 3 h to 17 h after injection, indicating a high stability of this bisphosphonate in bone tissue. This preliminary study implies that pharmacokinetics, biological activity and clinical applications of amidebisphosphonates in general, and the described compound in particular, should be further evaluated. © 1998 John Wiley & Sons, Ltd.