Preparation and in vivo binding of [11C]carazolol, a radiotracer for the beta-adrenergic receptor.
Carazolol is a high affinity beta-adrenergic receptor antagonist which is relatively non-specific for the receptor subtypes. The labeling of the two enantiomers of this compound with carbon-11, including the synthesis of the required labeling precursors, is reported. The yield and specific activity are sufficient for use in positron tomography. Biodistribution and specific receptor binding studies show the labeled material to be of interest for further investigation as a radiopharmaceutical for positron tomography.
Department of Radiology and Chemistry, Case Western Reserve University, Cleveland, OH 44106.
M S
MS
Berridge
E H
EH
Cassidy
A H
AH
Terris
J M
JM
Vesselle
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D000818:Animals; D002250:Carbon Radioisotopes; D007275:Injections, Intravenous; D007553:Isotope Labeling / Q000379:methods*; D008297:Male; D051379:Mice; D011412:Propanolamines / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D014018:Tissue Distribution
D000319:Adrenergic beta-Antagonists; D002250:Carbon Radioisotopes; D011412:Propanolamines; C014382:carazolol