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Title: Characterization of beta-adrenoreceptors in vivo with iodine-131 pindolol and gamma scintigraphy

Abstract

The aim of this study to was to assess the feasibility of using iodopindolol to delineate myocardial beta-adrenoreceptors in vivo. Preliminary biodistribution studies indicated that binding of /sup 131/I-d,I-pindolol in the heart was stereospecific, saturable, and displaceable by I-propranolol but not by phenoxybenzamine. However, considerable nonspecific binding was encountered. Subsequently, the stereoisomer, /sup 131/I-I-pindolol, was shown to be a high affinity beta-adrenoreceptor antagonist (Kd approximately 0.37 nM) as assessed by Scatchard analysis, and one exhibiting marked specific uptake in lung and heart in rabbits. In contrast, /sup 131/I-d-pindolol exhibited no specific binding in rabbit left ventricular membrane preparations nor specific organ uptake. Gamma camera scintigraphy with both isomers demonstrated that the I-isomer accumulated in lung and heart, and that its accumulation was blocked by I-propranolol. In contrast, d-isomer uptake was nonspecific and diffuse. The results indicate that it should be possible to externally visualize receptors by differentiating specific and nonspecific binding components of a ligand in vivo with the use of radiolabeled stereoisomers.

Authors:
; ; ;
Publication Date:
Research Org.:
Washington Univ. School of Medicine, St. Louis, MO
OSTI Identifier:
5207507
Resource Type:
Journal Article
Journal Name:
J. Nucl. Med.; (United States)
Additional Journal Information:
Journal Volume: 5
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; ADRENALINE; RECEPTORS; MYOCARDIUM; SCINTISCANNING; CELL MEMBRANES; IODINE 131; RABBITS; RATS; TISSUE DISTRIBUTION; ADRENAL HORMONES; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BODY; CARDIOTONICS; CARDIOVASCULAR AGENTS; CARDIOVASCULAR SYSTEM; CELL CONSTITUENTS; COUNTING TECHNIQUES; DAYS LIVING RADIOISOTOPES; DIAGNOSTIC TECHNIQUES; DISTRIBUTION; DRUGS; HEART; HORMONES; INTERMEDIATE MASS NUCLEI; IODINE ISOTOPES; ISOTOPES; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; MUSCLES; NEUROREGULATORS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANS; PROTEINS; RADIOISOTOPE SCANNING; RADIOISOTOPES; RODENTS; STEROID HORMONES; SYMPATHOMIMETICS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Hughes, B, Marshall, D R, Sobel, B E, and Bergmann, S R. Characterization of beta-adrenoreceptors in vivo with iodine-131 pindolol and gamma scintigraphy. United States: N. p., 1986. Web.
Hughes, B, Marshall, D R, Sobel, B E, & Bergmann, S R. Characterization of beta-adrenoreceptors in vivo with iodine-131 pindolol and gamma scintigraphy. United States.
Hughes, B, Marshall, D R, Sobel, B E, and Bergmann, S R. 1986. "Characterization of beta-adrenoreceptors in vivo with iodine-131 pindolol and gamma scintigraphy". United States.
@article{osti_5207507,
title = {Characterization of beta-adrenoreceptors in vivo with iodine-131 pindolol and gamma scintigraphy},
author = {Hughes, B and Marshall, D R and Sobel, B E and Bergmann, S R},
abstractNote = {The aim of this study to was to assess the feasibility of using iodopindolol to delineate myocardial beta-adrenoreceptors in vivo. Preliminary biodistribution studies indicated that binding of /sup 131/I-d,I-pindolol in the heart was stereospecific, saturable, and displaceable by I-propranolol but not by phenoxybenzamine. However, considerable nonspecific binding was encountered. Subsequently, the stereoisomer, /sup 131/I-I-pindolol, was shown to be a high affinity beta-adrenoreceptor antagonist (Kd approximately 0.37 nM) as assessed by Scatchard analysis, and one exhibiting marked specific uptake in lung and heart in rabbits. In contrast, /sup 131/I-d-pindolol exhibited no specific binding in rabbit left ventricular membrane preparations nor specific organ uptake. Gamma camera scintigraphy with both isomers demonstrated that the I-isomer accumulated in lung and heart, and that its accumulation was blocked by I-propranolol. In contrast, d-isomer uptake was nonspecific and diffuse. The results indicate that it should be possible to externally visualize receptors by differentiating specific and nonspecific binding components of a ligand in vivo with the use of radiolabeled stereoisomers.},
doi = {},
url = {https://www.osti.gov/biblio/5207507}, journal = {J. Nucl. Med.; (United States)},
number = ,
volume = 5,
place = {United States},
year = {Thu May 01 00:00:00 EDT 1986},
month = {Thu May 01 00:00:00 EDT 1986}
}