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 β 1-selective radioligands. A promising radioligand for imaging myocardial α 1-ARs, [ 11C]GB67, is now being evaluated in human PET experiments.

Original languageEnglish
Pages (from-to)191-200
Number of pages10
JournalPharmacochemistry Library
Volume31
Issue numberC
DOIs
Publication statusPublished - 2000

Fingerprint

Positron emission tomography
Positron-Emission Tomography
Adrenergic Receptors
Imaging techniques
Cardiomyopathies
Myocardial Ischemia
Myocardium
Norepinephrine
Heart Failure
Hypertension
Research

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Organic Chemistry

Cite this

Selection, design and evaluation of new radioligands for PET studies of cardiac adrenoceptors. / Pike, V. W.; Law, M. P.; Osman, S.; Davenport, R. J.; Rimoldi, O.; Giardinà, D.; Camici, P. G.

In: Pharmacochemistry Library, Vol. 31, No. C, 2000, p. 191-200.

Research output: Contribution to journalArticle

Pike, V. W. ; Law, M. P. ; Osman, S. ; Davenport, R. J. ; Rimoldi, O. ; Giardinà, D. ; Camici, P. G. / Selection, design and evaluation of new radioligands for PET studies of cardiac adrenoceptors. In: Pharmacochemistry Library. 2000 ; Vol. 31, No. C. pp. 191-200.
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