Synthesis of d-[11C]oxyphenonium iodide, a potential radioligand for in vivo visualization of human cholinergic muscarinic receptor-sites by positron emission tomography.
Carbon-11 labeled d-oxyphenonium iodide, a cholinergic antagonist is synthesized for in vivo visualization of muscarinic receptor-sites on airway tissue by positron emission tomography (PET). Methylation with [11C]CH3I of d-demethyloxyphenonium, followed by HPLC purification affords the desired radiopharmaceutical with a radiochemical yield of 66% (based on [11C]CH3I, and corrected for decay) and with a specific activity of 110-300 Ci/mmol. The biologically active labeled d-enantiomer is prepared within 40 min after EOB. Optical and chemical purity proved to be better than 99.9%. Radiochemical purity was determined to be higher than 99%.
Vlek
J W
JW
Department of Nuclear Medicine, University Hospital, The Netherlands.
Feitsma
K G
KG
van der Mark
T W
TW
Drenth
B F
BF
Paans
A M
AM
Vaalburg
W
W
D001665:Binding Sites; D002250:Carbon Radioisotopes; D006801:Humans; D007553:Isotope Labeling; D009130:Muscle, Smooth / Q000000981:diagnostic imaging*; D010115:Oxyphenonium / Q000138:chemical synthesis*; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis*; D011976:Receptors, Muscarinic / Q000378:metabolism; D012137:Respiratory System / Q000000981:diagnostic imaging; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D000644:Quaternary Ammonium Compounds; D011976:Receptors, Muscarinic; D010115:Oxyphenonium