Selection, design and evaluation of new radioligands for PET studies of cardiac adrenoceptors

V. W. Pike, M. P. Law, S. Osman, R. J. Davenport, O. Rimoldi, D. Giardinà, P. G. Camici

Research output: Contribution to journalArticle

Abstract

Changes in the numbers of human cardiac adrenoceptors (ARs) are associated with various diseases, such as myocardial ischemia, congestive heart failure, cardiomyopathy and hypertension. There is a clear need for capability to assess human cardiac ARs directly in vivo. Positron emission tomography (PET) is an imaging technique that provides this possibility, if effective radioligands can be developed for the targeted ARs. Here, the status of myocardial AR radioligand development for PET is described. Currently, there exist effective radioligands for imaging β-ARs in human myocardium. One of these, [11C](S)-CGP 12177, is applied extensively to clinical research with PET, sometimes with other tracers of other aspects of the noradrenalin system. Alternative radioligands are in development for β-ARs, including β1-selective radioligands. A promising radioligand for imaging myocardial α1-ARs, [11C]GB67, is now being evaluated in human PET experiments. Copyright (C) 2000 Elsevier Science B.V.

Original languageEnglish
Pages (from-to)191-200
Number of pages10
JournalPharmaceutica Acta Helvetiae
Volume74
Issue number2-3
DOIs
Publication statusPublished - Mar 2000

Keywords

  • Adrenoceptors
  • Carbon-11
  • Fluorine-18
  • Heart
  • Imaging
  • Positron emission tomography (PET)
  • Radioligands

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

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