Advancing 6-bromo-7-[¹¹C]methylpurine to clinical use: improved regioselective radiosynthesis, non-clinical toxicity data and human dosimetry estimates.

ABSTRACT:

Background

6-Bromo-7-[¹¹C]methylpurine ([¹¹C]BMP) is a radiotracer for positron emission tomography (PET) to measure multidrug resistance-associated protein 1 (MRP1) transport activity in different tissues. Previously reported radiosyntheses of [¹¹C]BMP afforded a mixture of 7- and 9-[¹¹C]methyl regioisomers. To prepare for clinical use, we here report an improved regioselective radiosynthesis of [¹¹C]BMP, the results of a non-clinical toxicity study as well as human dosimetry estimates based on mouse PET data.

Results

[¹¹C]BMP was synthesised by regioselective N⁷-methylation of 6-bromo-7H-purine (prepared under good manufacturing practice) with [¹¹C]methyl triflate in presence of 2,2,6,6

SUBMITTER: Mairinger S 

PROVIDER: S-EPMC11058743 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature