Receptor imaging in the thorax with PET

Eur J Pharmacol. 2004 Sep 19;499(1-2):1-13. doi: 10.1016/j.ejphar.2004.06.057.

Abstract

This review focuses on positron emission tomography (PET)-imaging of receptors in the sympathetic and the parasympathetic systems of heart and lung and highlights the human applications of PET. For the alpha-adrenoceptor, only [11C]GB67 (N2-[6-[(4-amino-6,7-dimethoxy-2-quinazolinyl)(methyl)amino]hexyl]-N2-[11C]methyl-2-furamide hydrochloride) has been developed. Its potential for application in patients needs to be assessed. For both the beta-adrenergic and the muscarinic systems, potent PET radioligands have been prepared and evaluated in patients. It has been possible to measure receptor densities quantitatively in human heart [[11C]MQNB: [11C]methylquinuclidinyl benzilate, [11C]CGP12177: S-(3'-t-butylamino-2'-hydroxypropoxy)-benzimidazol-2-[11C]one and [11C]CGP12388: (S)-4-(3-(2'-[11C]isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one] and qualitatively in lung [[11C]VC002: N-[11C]-methyl-piperidin-4-yl-2-cyclohexyl-2-hydroxy-2-phenylacetate and [11C]CGP12177]. Besides these subtype nonselective radioligands, the development of compounds that are selective for one subtype are ongoing and have not found successful application in humans yet.

Publication types

  • Review

MeSH terms

  • Adrenergic alpha-Agonists / metabolism
  • Adrenergic alpha-Antagonists / metabolism
  • Adrenergic beta-Agonists / metabolism
  • Adrenergic beta-Antagonists / metabolism
  • Animals
  • Benzimidazoles / metabolism
  • Carbazoles / metabolism
  • Carbon Radioisotopes
  • Ethanolamines / metabolism
  • Formoterol Fumarate
  • Humans
  • Positron-Emission Tomography / methods*
  • Propanolamines / metabolism
  • Radioligand Assay
  • Receptors, Adrenergic, alpha / metabolism*
  • Receptors, Adrenergic, beta / metabolism*
  • Thorax / diagnostic imaging*
  • Thorax / metabolism

Substances

  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Benzimidazoles
  • Carbazoles
  • Carbon Radioisotopes
  • Ethanolamines
  • Propanolamines
  • Receptors, Adrenergic, alpha
  • Receptors, Adrenergic, beta
  • CGP 12388
  • fluorocarazolol
  • CGP 12177
  • Formoterol Fumarate