Radiosynthesis of (N-[11C]methyl)benperidol for PET investigation of D2 receptor binding

Radiochimica Acta

Volumn 92, Issue 4-6, 2004, Pages 333-339

  Moerlein, Stephen M ^a   Perlmutter, Joel S ^a   Welch, Michael J ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

(N 11C methyl)benperidol; 11C NMB; Dopamine; Dopamine D2 receptors; PET; Radiopharmaceutical

Indexed keywords

BENPERIDOL; DOPAMINE 2 RECEPTOR; N METHYLBENPERIDOL C 11; UNCLASSIFIED DRUG;

ARTICLE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; METHYLATION; POSITRON EMISSION TOMOGRAPHY; PURIFICATION; QUALITY CONTROL; RECEPTOR BINDING; RELIABILITY;

EID: 3142744557     PISSN: 00338230     EISSN: None     Source Type: Journal    
DOI: 10.1524/ract.92.4.333.35584     Document Type: Article

References (35)

1. Stöcklin, G., Pike, V. W. (Eds.): Radiopharmaceuticals for Positron Emission Tomography. Methodological Aspects. Kluwer Academic Publishers, Boston, MA (1993).
2. Welch, M. J., Redvanly, C. S. (Eds.): Handbook of Radiopharmaceuticals. Radiochemistry and Applications. John Wiley and Sons, Inc., Hoboken, NJ (2003).
3. 11C-methyl-benperidol. J. Nucl. Med. 31, 2015 (1990).
4. Qaim, S. M., Clark, J. C., Crouzel, C., Guillaume, M., Helmeke, H. J., Pike, V. W., Stöcklin, G.: Radionuclide production. In: Radiopharmaceuticals for Positron Emission Tomography: Methodological Aspects. (Stocklin, G., Pike, V. W., eds.) Kluwer Academic Publishers, Boston, MA (1993).
5. Moerlein, S. M., Banks, W. R., Parkinson, D.: Production of fluorine-18 labeled (3-N-methyl)benperidol for PET investigation of cerebral dopaminergic receptor binding. Appl. Radiat. Isot. 43, 913 (1992).
6. Monograph 71. Sterility Tests. In: United States Pharmacopeia 27/National Formulary 22 (2004).
7. Monograph 85. Bacterial Endotoxins Test. In: United States Pharmacopeia 27/National Formulary 22 (2004).
8. Peroutka, S. J., Snyder, S. H.: Relationship of neuroleptic drug effects at brain dopamine, serotonin, α-adrenergic and histamine receptors to clinical potency. Am. J. Psychiatry 137, 1518 (1980).
9. Fachinformation, Glianimon® 2mg/5mg/10mg/Tropfen, benperidol. Bayer Vital GmbH & Co. KG, Leverkusen, 1997.
10. 75,77Br-brombenperidol. J. Lab. Comp. Radiopharm. 21, 875 (1984).
11. 77Br-brombenperidol in rat brain. Life Sci. 35, 1357 (1984).
12. 75Br-labelled butyrophenone neuroleptics for imaging of cerebral dopamine receptor areas using positron emission tomography. Eur. J. Nucl. Med. 12, 211 (1986).
13. 18F-labeled butyrophenone neuroleptic drugs in the baboon using positron emission tomography. J. Neurochem. 44, 835 (1985).
14. 18F-labeled ligand. Nucl. Med. Biol. 22, 809 (1995).
15. 18F]fluoroethyl)-benperidol to primate cerebral dopaminergic D2 receptors demonstrated in vivo by PET. Neurosci. Lett. 148, 97 (1992).
16. 18F](N-methyl)benperidol: a novel PET tracer for assessment of dopaminergic D2-like receptor binding. J. Cereb. Blood Flow Metab. 17, 833 (1997).
17. 11C]raclopride in the human brain. Synapse 16, 255 (1994).
18. 11C]raclopride at dopamine receptors in human subjects. Am. J. Psychiatry 154, 1209 (1997).
19. Perlmutter, J. S., Moerlein, S. M., Hwang, D.-R., Todd, R.: Non-steady-state measurement of in vivo radioligand binding by positron emission tomography: specificity analysis and comparison with in vitro binding. J. Neurosci. 11, 1381 (1991).
20. Frost, J. J., Smith, A. C., Kuhar, M. J., Dannals, R. F., Wagner, H. N.: In vivo binding of 3H-N-methylspiperone to dopamine and serotonin receptors. Life Sci. 40, 987.
21. 18F](N-methyl)benperidol as determined by whole-body PET imaging of primates. Nucl. Med. Biol. 24, 311 (1997).
22. 11C]methane. Appl. Radiat. Isot. 48, 153 (1997).
23. 2. Nucl. Med. Biol. 24, 93 (1997).
24. Dence, C. S., Margenau, W., Lee, H., Bognar, C., Moerlein, S. M., Al-Qahtani, M., Welch, M. J.: GE PETtrace MeI Microlab: six years' experience with system. Book of Abstracts. Ninth International Workshop on Targetry and Target Chemistry, Turku, Finland, May 23-25 (2002) E06.
25. 11C]methyl iodide. Appl. Radiat. Isot. 38, 601 (1987).
26. 11C]methyl)spiperone. Appl. Radiat. Isot. 37, 433 (1986).
27. 11C]methylspiperone with high specific activity and high radiochemical purity for PET studies: suppresion of its radiolysis. Appl. Radiat. Isot. 41, 593 (1990).
28. 11C]Methyl)spiperone, a ligand binding to dopamine receptors: radiochemical synthesis and biodistribution studies in mice. J. Nucl. Med. 25, 1222 (1984).
29. Raclopride C 11 Injection. In: United States Pharmacopeia 27/National Formulary 22 (2004).
30. Meyer, G.-J., Coenen, H. H., Waters, S. L., Långström, B., Cantineau, R., Stijckmans, K., Vaalburg, W., Halldin, C., Crouzel, C., Mazière, B., Luxen, A.: Quality assurance and quality control of short-lived radiopharmaceuticals for PET. In: Radiopharmaceuticals for Positron Emission Tomography: Methodological Aspects. (Stöcklin, G., Pike, V. W., eds.) Kluwer Academic Publishers, Boston, MA (1993).
31. Perlmutter, J. S., Moerlein, S. M., Welch, M. J.: Imaging studies of [C-11](N-methyl)benperidol (NMB) as a D2 receptor-binding PET tracer. Soc. Neurosci. Abstr. (2001) Abstr. 373.3.
32. Moerlein, S. M., Franquiz, J., Antenor, J., Welch, M. J., Perlmutter, J. S.: Absorbed radiation dosimetry of the PET D2 radioligand N-([C-11]methyl) benperidol ([C-11]NMB). Soc. Neurosci. Abstr. (2003) Abstr. 21.7.
33. Moerlein, S. M., Perlmutter, J. S., Engelbach, J., Sharp, T., Kim, J. Y., Rowland, D., LaForest, R., Mody, P., Patel, G., Lechner, K., Welch, M. J.: Comparison of carbon-11 and fluorine-18 labeled (N-methyl)benperidol (NMB) in rodents using Micro-PET imaging. J. Lab. Compd. Radiopharm. 44, S455 (2001).
34. Moerlein, S. M., Perlmutter, J. S., Kim, J. Y., Engelbach, J., Sharp, T., LaForest, R., Welch, M. J.: High-resolution imaging of neuroreceptor activity in living rodents using MicroPET. Book of Abstracts. High Resolution Imaging in Small Animals: Instrumentation, Applications and Animal Handling. Rockville, MD, Sep. 9-11 (2001) pp. 233-235.
35. Moerlein, S. M., Perlmutter, J. S., Tal, Y. C., Laforest, R., Antenor, J., Shockley, S. E., Welch, M. J.: Imaging of cerebral D2 receptor binding in living primates using the MicroPET Focus scanner. Mol. Imaging Biol. 5, 117 (2003).