𝔖 Bobbio Scriptorium
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Synthesis and biodistribution of acetyl-3,5-br-82-dibromosalicylic acid

✍ Scribed by Steven H. Wong; Richard P. Spencer


Publisher
John Wiley and Sons
Year
1981
Tongue
French
Weight
375 KB
Volume
18
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

Acetyl‐3,5‐Br‐82‐dibromosalicylic acid (dibromoaspirin) was synthesized by radiobromination of salicylic acid to yield 3,5‐dibromosalicylic acid, followed by acetylation of this intermediate. Biodistribution studies in mice with and without a neuroblastoma showed that the tumor/blood radioactivity ratio was low (0.3 at one hour). Thin layer chromatography of urine indicated that only 20 to 30% of the radioactivity corresponded to dibromoaspirin. Studies of rabbits with inflammatory lesions showed that the inflammatory/normal tissue uptake ratio was 1.0 to 1.9. The RBC/plasma ratio was less than 0.5. Low uptake of radioactivity was likely due to rapid dehalogenation in vivo.


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