Simple and fully automated preparation of [carbonyl-11C]WAY-100635

So far, [carbonyl-11C]WAY-100635 is the PET-tracer of choice for 5HT1A-receptor-imaging. Since the preparation is still a challenge, we aimed at (1) the evaluation of various essential parameters for the successful preparation, (2) the simplification of the radiosynthesis and (3) the establishment of a safe and fully automated system. The preparation is based on a commercial synthesizer and all chemicals are used without further processing. We found a low failure rate (7.7%), high average yield (4.0 ± 1.0 GBq) and a specific radioactivity of 292 ± 168 GBq/μmol (both at the end of synthesis, EOS).

[1]  F. Fazio,et al.  Automation of [11C]acyl chloride syntheses using commercially available 11C-modules. , 2002, Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine.

[2]  Wolfgang Wadsak,et al.  Reduced Serotonin-1A Receptor Binding in Social Anxiety Disorder , 2007, Biological Psychiatry.

[3]  P. Grasby,et al.  Characterisation of the appearance of radioactive metabolites in monkey and human plasma from the 5-HT1A receptor radioligand, [carbonyl-11C]WAY-100635--explanation of high signal contrast in PET and an aid to biomathematical modelling. , 1998, Nuclear medicine and biology.

[4]  Alan A. Wilson,et al.  Solid-phase radiosynthesis of [11C]WAY 100635 , 1996 .

[5]  Jan Passchier,et al.  Visualisation of serotonin-1A (5-HT1A) receptors in the central nervous system , 2001, European Journal of Nuclear Medicine.

[6]  A Malizia,et al.  First delineation of 5-HT1A receptors in human brain with PET and [11C]WAY-100635. , 1995, European journal of pharmacology.

[7]  M. Mintun,et al.  [11C]WAY 100635: a radioligand for imaging 5-HT1A receptors with positron emission tomography. , 1994, Life sciences.

[8]  S. Houle,et al.  Imaging the 5-HT(1A) receptors with PET: WAY-100635 and analogues. , 2000, Nuclear medicine and biology.

[9]  Victor W. Pike,et al.  Remotely-controlled production of the 5-HT1A receptor radioligand, [carbonyl-11C]WAY-100635, via 11C-carboxylation of an immobilized Grignard reagent , 1996 .

[10]  D. Hwang,et al.  An improved one-pot procedure for the preparation of [11C-carbonyl]-WAY100635. , 1999, Nuclear medicine and biology.

[11]  I. Cliffe,et al.  A retrospect on the discovery of WAY-100635 and the prospect for improved 5-HT(1A) receptor PET radioligands. , 2000, Nuclear medicine and biology.

[12]  P A Sargent,et al.  Exquisite delineation of 5-HT1A receptors in human brain with PET and [carbonyl-11 C]WAY-100635. , 1996, European journal of pharmacology.

[13]  A A Lammertsma,et al.  Evaluation of [O-methyl-3H]WAY-100635 as an in vivo radioligand for 5-HT1A receptors in rat brain. , 1994, European journal of pharmacology.