[123/131I]Iodometomidate as a radioligand for functional diagnosis of adrenal disease: synthesis, structural requirements and biodistribution
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| 024 | 7 | 0 | |a 10.1524/ract.92.4.297.35598 |2 doi |
| 035 | |a (NATIONALLICENCE)gruyter-10.1524/ract.92.4.297.35598 | ||
| 245 | 0 | 0 | |a [123/131I]Iodometomidate as a radioligand for functional diagnosis of adrenal disease: synthesis, structural requirements and biodistribution |h [Elektronische Daten] |c [A. Schirbel, I. Zolle, F. Hammerschmidt, M. L. Berger, D. Schiller, H. Kvaternik, Chr. Reiners] |
| 520 | 3 | |a Metomidate [(R)-1-(1-phenylethyl)-1H-imidazole-5-carboxylic acid methyl ester] (MTO, 1, Fig.1) is a potent and selective inhibitor of the cytochrome P-450 enzyme system in the adrenal cortex. Labelled in the 4-position with radioiodine, (R)-4-[131I]iodometomidate, 2, [131I]IMTO has been evaluated by in-vitro studies and also ex-vivo in rats. [131I]IMTO was synthesized by oxidative radioiododestannylation using a suitable precursor which was prepared by a new stereoselective synthesis. Optimization of the labelling reaction was performed by systematic variation of the most important reaction parameters. Under optimum reaction conditions, a labelling yield of 95% was obtained. In-vitro-stability of the tracer was studied over 8days, indicating slow deiodination (0.27%/h). Displacement studies using [131I]IMTO and rat adrenal membranes revealed the structural requirements for high affinity binding, namely an intact ester group and (R)-configuration of the radioligand. Pharmacokinetic studies in rats showed fast accumulation of [131I]IMTO in the adrenals (approx. 10% ID/g tissue) with an activity plateau for 2hours. Metabolic degradation was indicated by a steady increase of renal activity up to 4hours post injection. Based on target to non-target ratios the highest contrast for imaging of the adrenals was observed between 30 and 60min post injection of [131I]IMTO. We conclude that SPECT using [123I]IMTO will be a promising method for the characterization of adrenal incidentalomas. | |
| 540 | |a © 2004 Oldenbourg Wissenschaftsverlag GmbH | ||
| 690 | 7 | |a Laboratory techniques, experiments |2 nationallicence | |
| 690 | 7 | |a Analytical chemistry |2 nationallicence | |
| 690 | 7 | |a Inorganic chemistry |2 nationallicence | |
| 700 | 1 | |a Schirbel |D A. |4 aut | |
| 700 | 1 | |a Zolle |D I. |4 aut | |
| 700 | 1 | |a Hammerschmidt |D F. |4 aut | |
| 700 | 1 | |a Berger |D M. L. |4 aut | |
| 700 | 1 | |a Schiller |D D. |4 aut | |
| 700 | 1 | |a Kvaternik |D H. |4 aut | |
| 700 | 1 | |a Reiners |D Chr |4 aut | |
| 773 | 0 | |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology |d Oldenbourg Wissenschaftsverlag GmbH |g 92/4-6/2004(2004-04-01), 297-303 |x 0033-8230 |q 92:4-6/2004<297 |1 2004 |2 92 |o ract | |
| 856 | 4 | 0 | |u https://doi.org/10.1524/ract.92.4.297.35598 |q text/html |z Onlinezugriff via DOI |
| 908 | |D 1 |a research article |2 jats | ||
| 950 | |B NATIONALLICENCE |P 856 |E 40 |u https://doi.org/10.1524/ract.92.4.297.35598 |q text/html |z Onlinezugriff via DOI | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Schirbel |D A. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Zolle |D I. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Hammerschmidt |D F. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Berger |D M. L. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Schiller |D D. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Kvaternik |D H. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Reiners |D Chr |4 aut | ||
| 950 | |B NATIONALLICENCE |P 773 |E 0- |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology |d Oldenbourg Wissenschaftsverlag GmbH |g 92/4-6/2004(2004-04-01), 297-303 |x 0033-8230 |q 92:4-6/2004<297 |1 2004 |2 92 |o ract | ||
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| 898 | |a BK010053 |b XK010053 |c XK010000 | ||
| 949 | |B NATIONALLICENCE |F NATIONALLICENCE |b NL-gruyter | ||