Synthesis of some 11C-labelled MAO-A inhibitors and their in vivo uptake kinetics in rhesus monkey brain

Nuclear Medicine and Biology

Volumn 24, Issue 5, 1997, Pages 381-388

  Bergström, Mats ^a,c   Westerberg, Göran ^a   Kihlberg, Tor ^a,b   Långström, Bengt ^a,b  

^a UPPSALA UNIVERSITY   (Sweden)

^b UPPSALA UNIVERSITY   (Sweden)

^c UPPSALA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

Brofaromine; Clorgyline; Hatmine; MAO A; Positron emission tomography

Indexed keywords

BROFAROMINE; CARBON 11; CGP 035748A; CLORGYLINE; HARMALINE; HARMALOL; HARMINE; MONOAMINE OXIDASE INHIBITOR; NORBROFAROMINE; UNCLASSIFIED DRUG; CARBON; DIAGNOSTIC AGENT;

ALKYLATION; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG LABELING; DRUG SYNTHESIS; ENZYME BINDING; ISOTOPE LABELING; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; ANIMAL; BRAIN; COMPUTER ASSISTED EMISSION TOMOGRAPHY; MACACA; METABOLISM; SYNTHESIS;

ANIMALS; BRAIN; CARBON RADIOISOTOPES; MACACA MULATTA; MONOAMINE OXIDASE INHIBITORS; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 85047676916     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(97)80003-0     Document Type: Article

References (21)

1. Da Prada M., Kettler R., Keller H. H., Burkard W. P. and Haefely W. E. (1989) Preclinical profiles of the novel reversible MAO-A inhibitors, moclobemide and brofaromine, in comparison with irreversible MAO inhibitors. J. Neural. Transm. Suppl. 28, 5-20.
2. 3H-Ro 19-6327 in vitro: Localization and abundance of MAO-A and MAO-B in rat CNS, peripheral organs, and human brain. J. Neurosci. 12, 1977-1999.
3. MacGregor R. R., Fowler J. S., Wolf A. P., Halldin C. and Långstrom B. (1988) Synthesis of suicide inhibitors of monoamine oxidase: Carbon-11-labelled chlorgyline, L-deprenyl and D-deprenyl. J. Label. Compd. Radiopharm. 25, 1.
4. 11C)deprenyl and dynamic positron emission tomography. J. Cereb. Blood Flow Metab. 11, 545-556.
5. Bench C. J., Price G. W., Lammertsma A. A., Cremer J. C., et al (1991) Measurement of human cerebral monoamine oxidase type B (MAO-B) activity with positron emission tomography (PET): A dose ranging study with the reversible inhibitor Ro 19-6327. Eur. J. Clin. Pharmacol. 40, 169-173.
6. Fowler J. S., Volkow N. D., Logan J., Schluer D. J. et al. (1993) Monoamine oxidase B (MAO B) inhibitor therapy in Parkinson's disease: The degree and reversibility of human brain MAO B inhibition by Ro 19 6327. Neurology 43, 1984-1992.
7. 11C]-brofaromine, a potential tracer for measuring MAO-A activity with PET. Eur. J. Nucl. Med. 21, 876 (Abstract).
8. 76Br]-brofaromine for PET studies of MAO-A activity. Proceedings of the Eleventh International Symposium on Radiopharmaceutical Chemistry, Vancouver, Canada, pp. 232-233.
9. Hirata M., Magata Y., Ohmomo Y., Saji H., Murakami K., Takagaki T. et al. (1995) Evaluation of radioiodonated iodoclorgyline as a SPECT radiopharmaceutical for MAO-A of the brain. Nucl. Med. Biol. 22, 175-180.
10. 11C)methionine. J. Nucl. Med. 28, 1037.
11. Bjurling, P., Reineck R., Westerberg G., Gee A. D., Sutcliffe J. and Långström B. (1995, August). SYNTHIA, a compact radiochemistry system for automated production of radiopharmaceuticals. Proceedings from the Sixth Workshop on Targetry and Target Chemistry, Vancouver, Canada.
12. Långström B. and Lundqvist H. (1979) A β-particle flow detector for liquid chromatography. J. Radioanal. Radiochem. Lett. 41, 375.
13. Kops E. R., Herzog H., Schmid A., Holte S. and Feinendegen L. E. (1990) Performance characteristics of an eight-ring whole-body PET scanner. J. Comput. Assist. Tomogr. 14 (3), 437-445.
14. 3H)Harmaline distribution in monkey brain: Pharmacological and autoradiographic study. Brain Res. 22, 391-396.
15. 3H)Harmaline as a specific ligand of MAO A: I. Properties of the active site of MAO-A from rat and bovine brains. J. Neurochem. 32, 1817-1827.
16. 3H)Harmaline as a specific ligand of MAO-A: II. Measurement of the turnover rates of MAO-A during ontogenesis in the rat brain. J. Neurochem. 32, 1829-1836.
17. Anderson M. C., Waldmeier P. C. and Tipton K. F. (1991) The inhibition of monoamine oxidase by brofaromine. Biochem. Pharmacol. 41, 1871-1877.
18. 3H)Harman binding experiments: I. A reversible and selective radioligand for monoamine oxidase subtype A in the CNS of the rat. J. Neurochem. 56, 490-499.
19. 3H)harman binding and monoamine oxidase subtypes A and B activity in marmoset and rat. J. Neurochem. 56, 500-508.
20. Möller H-J. and Waldmeier P. (1991) Brofaromine - a selective, revesible and short-acting MAO-A inhibitor: Review of the pharmacological and clinical findings. Pharmacopsychiatry 24, 50-54.
21. 3H)brofaromine to monoamine oxidase A in vivo: Displacement by clorgyline and moclobemide. Eur. J. Pharmacol. 180, 297-304.