Mapping the Cerebral Monoamine Oxidase Type A: Positron Emission Tomography Characterization of the Reversible Selective Inhibitor [ 11 C]Befloxatone
The Journal of Pharmacology and Experimental Therapeutics, ISSN: 0022-3565, Vol: 305, Issue: 2, Page: 467-473
2003
- 33Citations
- 23Captures
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Metrics Details
- Citations33
- Citation Indexes33
- 33
- CrossRef27
- Captures23
- Readers23
- 23
Article Description
Befloxatone is a competitive and reversible inhibitor of monoamine oxidase-A (MAOI-A). The aim of the study was to characterize the in vivo properties of [ 11 C]befloxatone and to validate its use as a ligand for the study of MAO-A by positron emission tomography (PET). PET studies were performed in baboons after i.v. injection of [ 11 C]befloxatone (551 ± 70 MBq, i.e.14.9 ± 1.9 mCi). [ 11 C]Befloxatone enters rapidly in the brain with a maximum uptake at 30 min. Brain concentration of the tracer is high in thalamus, striatum, pons and cortical structures (1.5–1.8% of injected dose per 100 ml of tissue), and lower in cerebellum (1.07% injected dose/100 ml). Nonsaturable uptake, obtained after a pretreatment with a high dose of nonlabeled befloxatone (0.4 mg/kg), is very low and represents only 3% of the total uptake. Brain uptake of [ 11 C]befloxatone is not altered by a pretreatment of a high dose with lazabemide (0.5 mg/kg i.v.), a selective MAOI-B but is completely blocked by a pretreatment with moclobemide (MAOI-A; 10 mg/kg). This confirms, in vivo, the selectivity of befloxatone for type A MAO. [ 11 C]Befloxatone brain radioactivity was displaced by administration of unlabeled befloxatone (30 min after the tracer injection). The displacement of the tracer from its binding sites is dose-dependent, with an ID 50 of 0.02 mg/kg for all studied structures. These results indicate that [ 11 C]befloxatone will be an excellent probe for the study of MAO-A in humans using PET.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0022356524363062; http://dx.doi.org/10.1124/jpet.102.046953; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=0037405749&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/12606609; https://linkinghub.elsevier.com/retrieve/pii/S0022356524363062; https://dx.doi.org/10.1124/jpet.102.046953; https://jpet.aspetjournals.org/content/305/2/467
Elsevier BV
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