Ligands for SPECT and PET imaging of muscarinic-cholinergic receptors of the heart and brain

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Interest in the potential use of cerebral SPECT and PET imaging for determination of the density and activity of muscarinic-cholinergic receptors (mAChR) has been stimulated by the changes in these receptors which occur in many neurological diseases. In addition, the important involvement of mAChR in modulating negative inotropic cardiac activity suggests that such receptor ligands may have important applications in evaluation of changes which may occur in cardiac disease. In this paper, the properties of several key muscarinic receptor ligands being developed or which have been used for clinical SPECT and PET are discussed. In addition, the ORNL development of ... continued below

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36 p.

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Knapp, F.F. Jr.; McPherson, D.W. & Luo, H. June 1, 1995.

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Description

Interest in the potential use of cerebral SPECT and PET imaging for determination of the density and activity of muscarinic-cholinergic receptors (mAChR) has been stimulated by the changes in these receptors which occur in many neurological diseases. In addition, the important involvement of mAChR in modulating negative inotropic cardiac activity suggests that such receptor ligands may have important applications in evaluation of changes which may occur in cardiac disease. In this paper, the properties of several key muscarinic receptor ligands being developed or which have been used for clinical SPECT and PET are discussed. In addition, the ORNL development of the new iodinated IQNP ligand based on QNB and the results of in vivo biodistribution studies in rats, in vitro competitive binding studies and ex vivo autoradiographic experiments are described. The use of radioiodinated IQNP may offer several advantages in comparison to IQNB because of its easy and high yield preparation and high brain uptake and the potential usefulness of the {open_quotes}partial{close_quotes} subtype selective IONP isomers. We also describe the development of new IQNP-type analogues which offer the opportunity for radiolabeling with positron-emitting radioisotopes (carbon-11, fluorine-18 and bromine-76) for potential use with PET.

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36 p.

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OSTI as DE95012870

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  • 5. Mediterranean symposium on nuclear medicine and radiopharmaceuticals - receptors, Athens (Greece), 23-28 May 1995

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  • Other: DE95012870
  • Report No.: CONF-9505232--1
  • Grant Number: AC05-84OR21400;FG05-88ER60649
  • Office of Scientific & Technical Information Report Number: 82386
  • Archival Resource Key: ark:/67531/metadc785862

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  • June 1, 1995

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  • Dec. 3, 2015, 9:30 a.m.

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  • Oct. 4, 2017, 2:07 p.m.

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Knapp, F.F. Jr.; McPherson, D.W. & Luo, H. Ligands for SPECT and PET imaging of muscarinic-cholinergic receptors of the heart and brain, article, June 1, 1995; Tennessee. (digital.library.unt.edu/ark:/67531/metadc785862/: accessed December 17, 2017), University of North Texas Libraries, Digital Library, digital.library.unt.edu; crediting UNT Libraries Government Documents Department.