Development of [11C]L-159,884: a radiolabelled, nonpeptide angiotensin II antagonist that is useful for angiotensin II, AT1 receptor imaging

Appl Radiat Isot. 1996 Feb;47(2):211-8. doi: 10.1016/0969-8043(95)00273-1.

Abstract

[11C]L-159,884 ([11C] N-[[4'[(2-ethyl-5,7-dimethyl-3H- imidazo[4,5-b]pyridin-3-yl) methyl] [1,1'-biphenyl]-2-yl] sulfonyl]-4-methoxybenzamide) and [11C]L-162,574 ([11C] N-[[4'[2-ethyl-5,7- dimethyl-3H-imidazo[4,5-b] pyridin-3-yl)methyl] [1,1'-biphenyl]-2-yl]sulfonyl]-3- methoxybenzamide), both potent and selective ligands for the AT1 receptor, were prepared by C-11 methylation of the corresponding desmethyl phenolic precursors. The radiotracers were purified by semi-preparative reverse-phase HPLC. Non-decay corrected radiochemical yields were 5 and 3% for L-159,884 and L-162,574 respectively, and the average specific activity was 2979 mCi/mumol at end-of-synthesis (EOS). The average time of synthesis was 18 min.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Angiotensin I / metabolism*
  • Angiotensin II / antagonists & inhibitors*
  • Angiotensin Receptor Antagonists
  • Carbon Radioisotopes / chemistry*
  • Chromatography, High Pressure Liquid
  • Hydrocarbons, Iodinated / chemistry
  • Image Processing, Computer-Assisted
  • Imidazoles / chemical synthesis
  • Imidazoles / metabolism*
  • Isotope Labeling / methods
  • Pyridines / chemical synthesis
  • Pyridines / metabolism*
  • Receptors, Angiotensin / metabolism*
  • Tomography, Emission-Computed

Substances

  • Angiotensin Receptor Antagonists
  • Carbon Radioisotopes
  • Hydrocarbons, Iodinated
  • Imidazoles
  • L 162574
  • Pyridines
  • Receptors, Angiotensin
  • Angiotensin II
  • L 159884
  • Angiotensin I
  • methyl iodide