Sodium-Proton Exchanger Isoform-1: Synthesis of a Potent Inhibitor Labeled with Deuterium and Carbon-14

Author(s): Bachir Latli, Nizar Haddad, Matt Hrapchak, Xudong Wei, Wenjun Tang, Jinhua J. Song, Chris H. Senanayake

Journal Name: Current Radiopharmaceuticals

Volume 6 , Issue 1 , 2013

Become EABM
Become Reviewer

Abstract:

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 1inhibitor 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 [14C]-(1) in three steps, with a specific activity of 55.6 mCi/mmol.

Keywords: NHE-1, Radiosynthesis, Carbon-14, deuterium, Comins reaction

promotion: free to download

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 6
ISSUE: 1
Year: 2013
Published on: 19 March, 2013
Page: [7 - 11]
Pages: 5
DOI: 10.2174/1874471011306010002

Article Metrics

PDF: 35