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Structure biodistribution relationship of radiolabeled ergolines: Search for brain imaging radiopharmaceuticals
Author(s) -
Basmadjian G. P.,
Sadek S. A.,
Mikhail E. A.,
Parikh A.,
Weaver A.,
Mills S. L.
Publication year - 1989
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580270803
Subject(s) - pergolide , chemistry , biodistribution , moiety , agonist , radiosynthesis , stereochemistry , dopamine , pharmacology , dopamine agonist , biochemistry , medicine , nuclear medicine , in vitro , receptor , positron emission tomography
A series of ergoline derivatives, analogues of Pergolide 1 and Lysergol 6 , were synthesized, radiolabeled with 125 I or 75 Se, and evaluated for their ability to cross the Blood Brain Barrier of rats, for potential use as radiopharmaceuticals for imaging the brain. Introduction of the radiolabel was either at the 17‐ position (attached to the 8β‐methylene) or at the 2‐ position of the indole portion of the ergoline moiety. Of the 8 radiolabeled compounds tested, two pergolide analogues, 8β‐(methyl‐ 75 Seseleno)‐methyl‐6‐propyl ergoline 5 and 8β−[ 125 I]‐iodomethyl‐6‐propyl ergoline 2f showed the highest uptake in the brain, adrenal and heart with good organ to blood ratios. This work has shown that analogues of pergolide, a dopamine agonist, if labeled with 123 I may yield a clinically useful brain imaging radiopharmaceutical.