Synthesis of radiotracers for studying muscarinic cholinergic receptors in the living human brain using positron emission tomography: [11C]dexetimide and [11C]levetimide.
Dexetimide (Fig. 1a), a potent muscarinic cholinergic receptor antagonist, and levetimide (Fig. 1b), its pharmacologically inactive enantiomer, were labeled with 11C for non-invasive in vivo studies of muscarinic cholinergic receptors in the human brain using positron emission tomography. The syntheses were completed in approximately 32 min using [alpha-11C]benzyl iodide as the precursor. The synthesis, purification, characterization and determination of specific activity are presented and discussed.
Dannals
R F
RF
Divisions of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.
Långström
B
B
Ravert
H T
HT
Wilson
A A
AA
Wagner
H N
HN
D001921:Brain / Q000000981:diagnostic imaging*; D002250:Carbon Radioisotopes; D003909:Dexetimide / Q000138:chemical synthesis*; D006801:Humans; D010880:Piperidines / Q000138:chemical synthesis*; D011976:Receptors, Muscarinic / Q000032:analysis*; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D010880:Piperidines; D011976:Receptors, Muscarinic; C018580:levetimide; D003909:Dexetimide