A novel radioligand for imaging the AT1 angiotensin receptor with PET.
2-Butyl-5-methoxymethyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine (KR31173) was radiolabeled by coupling a tetrazole-protected hydroxy precursor with [(11)C] methyl iodide and removing the protecting group by acid hydrolysis. In mice, the highest uptake of [(11)C] KR31173 was in the adrenal glands, kidneys, and liver. Tissue to blood ratios were generally greater than 10:1. Uptake of the tracer in the adrenal glands, kidneys, lungs, and heart was blocked with a 1 mg/kg dose of KR31173 or MK-996.
Mathews
William B
WB
Department of Radiology, Room B1151 Nelson Building, Johns Hopkins Medical Institutions, 600 North Wolfe St., Baltimore, MD 21287, USA. bmathews@petscan.nm.jhu.edu
Yoo
Sung-Eun
SE
Lee
Sung-Hou
SH
Scheffel
Ursula
U
Rauseo
Paige A
PA
Zober
Tamas G
TG
Gocco
Gerard
G
Sandberg
Kathryn
K
Ravert
Hayden T
HT
Dannals
Robert F
RF
Szabo
Zsolt
Z
D000311:Adrenal Glands / Q000000981:diagnostic imaging* / Q000378:metabolism*; D000818:Animals; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics; D007093:Imidazoles / Q000493:pharmacokinetics*; D007668:Kidney / Q000000981:diagnostic imaging* / Q000378:metabolism*; D008024:Ligands; D008099:Liver / Q000000981:diagnostic imaging* / Q000378:metabolism*; D008297:Male; D051379:Mice; D009928:Organ Specificity; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D044140:Receptor, Angiotensin, Type 1 / Q000378:metabolism*; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013777:Tetrazoles / Q000493:pharmacokinetics*; D014018:Tissue Distribution
C493912:2-butyl-5-methoxymethyl-6-(1-oxopyridin-2-yl)-3-((2'-(1H-tetrazol-5-yl)bipohenyl-4-yl)methyl)-3H-imidazo(4,5-b)pyridine; D002250:Carbon Radioisotopes; D007093:Imidazoles; D008024:Ligands; D019275:Radiopharmaceuticals; D044140:Receptor, Angiotensin, Type 1; D013777:Tetrazoles