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Radiosynthesis of [14C]acarbose
1Pharma Research Center, Bayer AG, Wuppertal, Fed. Rep. of Germany.
Arzneimittel-Forschung
|October 1, 1989
Summary
Radiolabeled acarbose was synthesized using D-[U-14C]glucose for pharmacokinetic studies. The [14C]carbon atoms were confirmed to be exclusively in the core structure of acarbose.
Area of Science:
- Biochemistry
- Pharmacology
- Organic Chemistry
Background:
- Acarbose is an alpha-glucosidase inhibitor used to treat diabetes mellitus.
- Investigating acarbose pharmacokinetics and biotransformation requires radiolabeled compounds.
- 14C-labeled acarbose ([14C]Bay g 5421) is essential for these studies.
Purpose of the Study:
- To synthesize 14C-labeled acarbose ([14C]Bay g 5421) for pharmacokinetic and biotransformation investigations.
- To determine the location of the incorporated 14C atoms within the acarbose molecule.
Main Methods:
- Fermentation of Actinoplanes mutant SN 1667/47 using D-[U-14C]glucose as a precursor under cometabolism with maltose.
- Purification and characterization of the synthesized [14C]acarbose.
- Hydrolysis of [14C]acarbose and analysis of its constituent parts.
Main Results:
- [14C]acarbose was obtained with a radiochemical yield of 1.58–2.56% and high radiochemical purity (>98%).
- Specific radioactivities ranged from 7.77 to 9.14 MBq/mg.
- Hydrolysis confirmed that the 14C label is localized exclusively in the core structure, not the maltose unit.
Conclusions:
- A reliable method for synthesizing 14C-labeled acarbose was established.
- The synthesis provides a crucial tool for future pharmacokinetic and metabolic studies of acarbose.
- Understanding the biotransformation pathway is vital for optimizing acarbose therapy.