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

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.
Authors:
; ;  [1]
  1. and others
Publication Date:
OSTI Identifier:
82386
Report Number(s):
CONF-9505232-1
ON: DE95012870; CNN: Grant No. NS-22215; TRN: 95:005166
DOE Contract Number:
AC05-84OR21400; FG05-88ER60649
Resource Type:
Conference
Resource Relation:
Conference: 5. Mediterranean symposium on nuclear medicine and radiopharmaceuticals - receptors, Athens (Greece), 23-28 May 1995; Other Information: PBD: [1995]
Research Org:
Oak Ridge National Lab., TN (United States); George Washington Univ., Washington, DC (United States)
Sponsoring Org:
USDOE, Washington, DC (United States); National Insts. of Health, Bethesda, MD (United States)
Country of Publication:
United States
Language:
English
Subject:
55 BIOLOGY AND MEDICINE, BASIC STUDIES; RADIOISOTOPES; UPTAKE; FEASIBILITY STUDIES; RECEPTORS; POSITRON COMPUTED TOMOGRAPHY; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY; CHOLINE; BRAIN; LIGANDS; RATS; HEART