Development of radioligands for the imaging of cardiac beta-adrenoceptors using SPECT .1. Asymmetric synthesis and structural characterization of five new iodine-containing beta-adrenoceptor antagonist derivatives

J.C. van den Bos, P.A.P.M. van Doremalen, E.A. Dubois, G.A. Somsen, J.A.J.M. Vekemans, A.G.M. Janssen, G.J. Boer, M. Pfaffendorf, E.A. van Royen, P.A. van Zwieten

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Abstract

The asymmetric synthesis of a series of iodinated beta-adrenoceptor ligands is described. One ligand, (S)-(-)-[1-(2-iodophenoxy)]-3'-(tert-butylamino)-2'-propanol (CYBL3), is based on the beta-adrenoceptor antagonist penbutolol. The other ligands are N-iodovinyl and N-iodoaryl analogues of the beta-adrenoceptor antagonist CGP12177. These have been synthesized from 2-amino-3-nitrophenol. Furthermore, radioiodinated [123I]CYBL3 and [123I](2'S,2"E)-[4-(3'-(1",1"-dimethyl-3"-iodo-2" propenylamino)-2'-hydroxy propoxy)]-benzimidazol-2-one have been prepared by radiolabelling the corresponding trialkyltin precursors using [123I]-NaI in the presence of hydrogen peroxide.
Original languageEnglish
Pages (from-to)1-7
Number of pages7
JournalNuclear Medicine and Biology
Volume24
Issue number1
DOIs
Publication statusPublished - Jan 1997

Keywords

  • CGP12177
  • penbutolol
  • beta-adrenoceptor
  • SPECT

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