Receptor binding radiotracers for the angiotensin II receptor: radioiodinated [Sar1, Ile8]Angiotensin II.
The potential for imaging the angiotensin II receptor was evaluated using the radioiodinated peptide antagonist [125I][Sar1, Ile8)angiotensin II. The radioligand provides a receptor-mediated signal in several tissues in rat (kidneys, adrenal and liver). The receptor-mediated signal of 3% ID/g kidney cortex should be sufficient to permit imaging, at least via SPECT. The radiotracer is sensitive to reductions in receptor concentration and can be used to define in vivo dose-occupancy curves of angiotensin II receptor ligands. Receptor-mediated images of [123I][Sar1, Ile8]angiotensin II were obtained in the rat kidney and Rhesus monkey liver.
Gibson
R E
RE
Department of Pharmacology, Merck Sharp & Dohme Research Laboratories, West Point, PA 19486, USA.
Beauchamp
H T
HT
Fioravanti
C
C
Brenner
N
N
Burns
H D
HD
D015059:1-Sarcosine-8-Isoleucine Angiotensin II / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D000311:Adrenal Glands / Q000378:metabolism / Q000648:ultrastructure; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000378:metabolism / Q000494:pharmacology; D001345:Autoradiography; D005260:Female; D007093:Imidazoles / Q000378:metabolism / Q000494:pharmacology; D007457:Iodine Radioisotopes; D007668:Kidney / Q000378:metabolism / Q000648:ultrastructure; D008099:Liver / Q000378:metabolism / Q000648:ultrastructure; D008253:Macaca mulatta; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D011945:Receptors, Angiotensin / Q000378:metabolism*; D013777:Tetrazoles / Q000378:metabolism / Q000494:pharmacology; D005466:Fluorocarbons
D015059:1-Sarcosine-8-Isoleucine Angiotensin II; D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D007093:Imidazoles; D007457:Iodine Radioisotopes; D011945:Receptors, Angiotensin; D013777:Tetrazoles; C099368:angiotensin II, iodo-(Sar(1)-Ile(8))-; C069045:DuP 532; D005466:Fluorocarbons; C070967:L 158809