Ohmomo, Yoshiro published the artcileRadioiodinated N-(2-aminoethyl)-2-chloro-4-iodobenzamide: a new ligand for monoamine oxidase B studies with single photon emission computed tomography, Synthetic Route of 145343-76-6, the publication is Chemical & Pharmaceutical Bulletin (1994), 42(4), 913-16, database is CAplus.
In developing monoamine oxidase (MAO)-B specific radioligands, N-(2-aminoethyl)-2-chloro-4-[125I]iodobenzamide ([125I]FIBA) was conveniently synthesized from its tributylstannyl precursor by an iodostannylation reaction using sodium [125I]iodide and hydrogen peroxide with high radiochem. yield. The method should be applicable for labeling with 125I, a suitable radioisotope for in vivo imaging with single photon emission computed tomog. (SPECT). In vitro binding studies using mouse brain mitochondrial preparations showed that the specific binding of [125I]FIBA was saturable and of high affinity. Calculated values for KD and Bmax were 201 nM and 2.5 pmol/mg protein, resp. The [125I]FIBA binding was effectively prevented by MAO-B specific inhibitors (l-deprenyl, Ro 16-6491, FIBA) or substrate (β-phenethylamine). However, MAO-A specific inhibitor (clorgyline) and substrate (serotonin) had no significant effect. After an i.v. injection into mice, [125I]FIBA showed high brain uptake (1.64% dose/g at 15-30 min postinjection) and long retention (1.11% dose/g at 120 min postinjection) in the brain. Good brain-to-blood radioactivity ratios of 2.19 and 2.41 at 60 and 120 min after injection, resp., were obtained. The in vitro binding data and in vivo characteristics suggested that [125I]FIBA is potentially useful as a probe for biol. studies including specific labeling of MAO-B in vivo as well as in vitro. Moreover, the 123I-labeled counterpart, [125I]FIBA, might be valuable for noninvasive imaging and mapping of MAO-B in the living brain with SPECT.
Chemical & Pharmaceutical Bulletin published new progress about 145343-76-6. 145343-76-6 belongs to iodides-buliding-blocks, auxiliary class Chloride,Iodide,Carboxylic acid,Benzene, name is 2-Chloro-4-iodobenzoic acid, and the molecular formula is C7H4ClIO2, Synthetic Route of 145343-76-6.
Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com