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Curr Radiopharm. 2013 Mar;6(1):7-11.

Sodium-proton exchanger isoform-1: synthesis of a potent inhibitor labeled with deuterium and carbon-14.

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  • 1Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc. 900 Ridgebury Road, Ridgefield, CT 06877 USA.


Sodium-proton exchangers, NHEs are plasma membrane proteins that are essential in the regulation of intracellular pH of the myocardium. There are nine known variously expressed isoforms of NHEs with NHE-1 being the predominant isoform in the heart. N-[4-(1-acetyl-piperidin-4-yl)-3-trifluoromethyl-benzoyl]-guanidine (1) is a potent NHE 1-inhibitor with good pharmacokinetics. It was prepared labeled with deuterium and carbon-14 to aid in drug metabolism, pharmacokinetics, and other studies. The combination of Comins' reaction and reduction under deuterium gas was used to access deuterium labeled (1) starting from deuterium labeled pyridine. Carbon-14 labeled zinc cyanide was used to prepare [(14)C]-(1) in three steps, with a specific activity of 55.6 mCi/mmol.

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