Preparation of [11C]- and [125I]IMB: a dopamine D-2 receptor antagonist.
A new dopamine D-2 receptor ligand, N-[2-(N'-4-iodobenzyl-N'-methyl)aminoethyl]-5-chloro-2-methoxy-4- (methylamino)benzamide (IMB) was synthesized and labelled with 11C and 125I at high specific activities. Both radiotracers were prepared by alkylation reactions with [11C]iodomethane and [125I]4-iodobenzyl bromide and appropriate 2 degrees amine precursors. Isolated radiochemical yields of 12-20% for [11C]IMB and 35-50% for [125I]IMB were achieved in 24 and 130-150 min respectively. [11C]IMB and [123I]IMB may prove suitable for a direct comparison of PET and SPECT in the localization and quantification of neuroreceptors.
Wilson
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Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.
Dannals
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Ravert
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Wagner
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D001549:Benzamides / Q000138:chemical synthesis*; D001921:Brain / Q000000981:diagnostic imaging; D002250:Carbon Radioisotopes; D018492:Dopamine Antagonists; D006801:Humans; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D011954:Receptors, Dopamine / Q000187:drug effects*; D014055:Tomography, Emission-Computed; D015899:Tomography, Emission-Computed, Single-Photon
D001549:Benzamides; D002250:Carbon Radioisotopes; D018492:Dopamine Antagonists; D007457:Iodine Radioisotopes; D011954:Receptors, Dopamine; C060906:spectramide