PMID: 9080468Jan 1, 1997Paper

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

Nuclear Medicine and Biology
J C van den BosP A van Zwieten


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.


Sep 17, 1976·The Journal of Organic Chemistry·L M WeinstockR Tull
Aug 1, 1977·Journal of Medicinal Chemistry·J J BaldwinA Scriabine
Jul 1, 1992·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·M S BerridgeJ M Vesselle
May 1, 1985·Journal of Neuroscience Methods·I A Macdonald, D M Lake
May 1, 1996·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·E A DuboisP A van Zwieten

Related Concepts

4-(3-tert-butylamino-2-hydroxypropoxy)benzimidazol-2-one, 2-(11)C-labeled
Adrenergic beta-Antagonists
Hydrocarbons, Iodinated
Radioligand Assay
Tomography, Emission-Computed, Single-Photon

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