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- W2076247192 abstract "In vivo evaluation of MAO-A would be of great value for the diagnosis and follow-up of therapy of depression. In order to perform this exploration by SPECT, we developed an iodinated derivative of the reversible MAO-A inhibitor, moclobemide. Ro 11-9900 was synthesized and analysed by IR, NMR and HPLC. Radioiodination was carried out by nucleophilic exchange of [ 125 I] on the brominated precursor, and yielded [ 125 I]-Ro 11–9900 with high specific activity. In vitro experiments on rat brain homogenates showed that Ro 11–9900 had poor inhibitory activity on MAO-A, as already described for moclobemide. By contrast, in vivo biodistribution in the rat brain showed that [ 125 I]-Ro 11–9900 accumulated in a region corresponding to the localization of locus coeruleus known for its high density of MAO-A. Moreover, preinjection of the irreversible MAO-A inhibitor clorgyline (10 mg. kg −1 ) prevented accumulation of radioactivity by 40 to 60% and we found that the radioactivity in the brain corresponded exclusively to [ 125 I]-Ro 11–9900 and not to a metabolite. [ 125 I]-Ro 11–9900 was highly accumulated in the pineal gland, both on MAO-A and on MAO-B sites. We concluded that the unmetabolized iodinated derivative of moclobemide, Ro 11–9900, preferentially labeled MAO-A in vivo in the rat brain. This compound would therefore be a potential tracer for evaluation of MAO-A by SPECT." @default.
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- W2076247192 date "1996-03-01" @default.
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- W2076247192 title "An iodinated derivative of moclobemide as potential radioligand for brain MAO-A exploration" @default.
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- W2076247192 doi "https://doi.org/10.1016/0024-3205(96)00074-4" @default.
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